JPS635384B2 - - Google Patents
Info
- Publication number
- JPS635384B2 JPS635384B2 JP53079271A JP7927178A JPS635384B2 JP S635384 B2 JPS635384 B2 JP S635384B2 JP 53079271 A JP53079271 A JP 53079271A JP 7927178 A JP7927178 A JP 7927178A JP S635384 B2 JPS635384 B2 JP S635384B2
- Authority
- JP
- Japan
- Prior art keywords
- hours
- pharmaceutically acceptable
- compounds
- treated
- base
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- 150000001875 compounds Chemical class 0.000 claims description 55
- 150000003839 salts Chemical class 0.000 claims description 18
- 239000002904 solvent Substances 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 11
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 9
- HGINCPLSRVDWNT-UHFFFAOYSA-N Acrolein Chemical compound C=CC=O HGINCPLSRVDWNT-UHFFFAOYSA-N 0.000 claims description 8
- 125000000219 ethylidene group Chemical group [H]C(=[*])C([H])([H])[H] 0.000 claims description 7
- JKANAVGODYYCQF-UHFFFAOYSA-N prop-2-yn-1-amine Chemical class NCC#C JKANAVGODYYCQF-UHFFFAOYSA-N 0.000 claims description 6
- 230000003287 optical effect Effects 0.000 claims description 5
- 230000008569 process Effects 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 230000007062 hydrolysis Effects 0.000 claims description 4
- 238000006460 hydrolysis reaction Methods 0.000 claims description 4
- DRUIESSIVFYOMK-UHFFFAOYSA-N Trichloroacetonitrile Chemical compound ClC(Cl)(Cl)C#N DRUIESSIVFYOMK-UHFFFAOYSA-N 0.000 claims description 3
- 150000001408 amides Chemical class 0.000 claims description 3
- MLUCVPSAIODCQM-NSCUHMNNSA-N crotonaldehyde Chemical compound C\C=C\C=O MLUCVPSAIODCQM-NSCUHMNNSA-N 0.000 claims description 3
- 229910052751 metal Inorganic materials 0.000 claims description 3
- 239000002184 metal Substances 0.000 claims description 3
- BGWBVEWXQAGTJL-UHFFFAOYSA-N 3,3,3-trichloropropanamide Chemical compound NC(=O)CC(Cl)(Cl)Cl BGWBVEWXQAGTJL-UHFFFAOYSA-N 0.000 claims description 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 2
- 238000005917 acylation reaction Methods 0.000 claims description 2
- 230000029936 alkylation Effects 0.000 claims description 2
- 238000005804 alkylation reaction Methods 0.000 claims description 2
- IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 claims description 2
- 239000011260 aqueous acid Substances 0.000 claims description 2
- 150000003857 carboxamides Chemical class 0.000 claims description 2
- 230000003197 catalytic effect Effects 0.000 claims description 2
- 150000001768 cations Chemical class 0.000 claims description 2
- MLUCVPSAIODCQM-UHFFFAOYSA-N crotonaldehyde Natural products CC=CC=O MLUCVPSAIODCQM-UHFFFAOYSA-N 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 150000004820 halides Chemical class 0.000 claims description 2
- 238000010438 heat treatment Methods 0.000 claims description 2
- 230000007935 neutral effect Effects 0.000 claims description 2
- 239000012454 non-polar solvent Substances 0.000 claims description 2
- ISHLCKAQWKBMAU-UHFFFAOYSA-N tert-butyl n-diazocarbamate Chemical compound CC(C)(C)OC(=O)N=[N+]=[N-] ISHLCKAQWKBMAU-UHFFFAOYSA-N 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 24
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 21
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 18
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 18
- 239000000243 solution Substances 0.000 description 18
- KIDHWZJUCRJVML-UHFFFAOYSA-N putrescine Chemical compound NCCCCN KIDHWZJUCRJVML-UHFFFAOYSA-N 0.000 description 16
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 14
- -1 aluminium Chemical class 0.000 description 13
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 10
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 description 9
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 9
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 9
- 229920000768 polyamine Polymers 0.000 description 9
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 9
- 239000005700 Putrescine Substances 0.000 description 8
- 239000002585 base Substances 0.000 description 8
- ATHGHQPFGPMSJY-UHFFFAOYSA-N spermidine Chemical compound NCCCCNCCCN ATHGHQPFGPMSJY-UHFFFAOYSA-N 0.000 description 8
- PFNFFQXMRSDOHW-UHFFFAOYSA-N spermine Chemical compound NCCCNCCCCNCCCN PFNFFQXMRSDOHW-UHFFFAOYSA-N 0.000 description 8
- 230000000694 effects Effects 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 6
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 6
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 6
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 6
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 6
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 description 6
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- 230000015572 biosynthetic process Effects 0.000 description 6
- 229910052744 lithium Inorganic materials 0.000 description 6
- 229960003104 ornithine Drugs 0.000 description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 5
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 5
- 239000005977 Ethylene Substances 0.000 description 5
- 239000002253 acid Substances 0.000 description 5
- 229960001570 ademetionine Drugs 0.000 description 5
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 5
- 230000012010 growth Effects 0.000 description 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 description 4
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 4
- 229920002261 Corn starch Polymers 0.000 description 4
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 description 4
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 description 4
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 4
- 241001465754 Metazoa Species 0.000 description 4
- MZRVEZGGRBJDDB-UHFFFAOYSA-N N-Butyllithium Chemical compound [Li]CCCC MZRVEZGGRBJDDB-UHFFFAOYSA-N 0.000 description 4
- MEFKEPWMEQBLKI-AIRLBKTGSA-N S-adenosyl-L-methioninate Chemical compound O[C@@H]1[C@H](O)[C@@H](C[S+](CC[C@H](N)C([O-])=O)C)O[C@H]1N1C2=NC=NC(N)=C2N=C1 MEFKEPWMEQBLKI-AIRLBKTGSA-N 0.000 description 4
- 150000001412 amines Chemical class 0.000 description 4
- 238000006243 chemical reaction Methods 0.000 description 4
- 239000008120 corn starch Substances 0.000 description 4
- 229940099112 cornstarch Drugs 0.000 description 4
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 description 4
- 244000005700 microbiome Species 0.000 description 4
- 239000003921 oil Substances 0.000 description 4
- 235000019198 oils Nutrition 0.000 description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 4
- 238000010992 reflux Methods 0.000 description 4
- 229910052708 sodium Inorganic materials 0.000 description 4
- 239000011734 sodium Substances 0.000 description 4
- 239000011780 sodium chloride Substances 0.000 description 4
- 229940063673 spermidine Drugs 0.000 description 4
- 229940063675 spermine Drugs 0.000 description 4
- 239000000725 suspension Substances 0.000 description 4
- 239000003826 tablet Substances 0.000 description 4
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- UAYWVJHJZHQCIE-UHFFFAOYSA-L zinc iodide Chemical compound I[Zn]I UAYWVJHJZHQCIE-UHFFFAOYSA-L 0.000 description 4
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 3
- 239000004475 Arginine Substances 0.000 description 3
- 229930186147 Cephalosporin Natural products 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 241000700159 Rattus Species 0.000 description 3
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 3
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 3
- 125000004432 carbon atom Chemical group C* 0.000 description 3
- 229940124587 cephalosporin Drugs 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 238000006114 decarboxylation reaction Methods 0.000 description 3
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- ARNWQMJQALNBBV-UHFFFAOYSA-N lithium carbide Chemical compound [Li+].[Li+].[C-]#[C-] ARNWQMJQALNBBV-UHFFFAOYSA-N 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 231100000252 nontoxic Toxicity 0.000 description 3
- 230000003000 nontoxic effect Effects 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 3
- UIIMBOGNXHQVGW-UHFFFAOYSA-M sodium bicarbonate Substances [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 3
- 235000011121 sodium hydroxide Nutrition 0.000 description 3
- 210000001519 tissue Anatomy 0.000 description 3
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 description 2
- NWZSZGALRFJKBT-KNIFDHDWSA-N (2s)-2,6-diaminohexanoic acid;(2s)-2-hydroxybutanedioic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O.NCCCC[C@H](N)C(O)=O NWZSZGALRFJKBT-KNIFDHDWSA-N 0.000 description 2
- FJJYHTVHBVXEEQ-UHFFFAOYSA-N 2,2-dimethylpropanal Chemical compound CC(C)(C)C=O FJJYHTVHBVXEEQ-UHFFFAOYSA-N 0.000 description 2
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 2
- SCNWTQPZTZMXBG-UHFFFAOYSA-N 2-methyloct-2-enoic acid Chemical compound CCCCCC=C(C)C(O)=O SCNWTQPZTZMXBG-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 description 2
- 241000283690 Bos taurus Species 0.000 description 2
- 241000282472 Canis lupus familiaris Species 0.000 description 2
- 239000004215 Carbon black (E152) Substances 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- XTHFKEDIFFGKHM-UHFFFAOYSA-N Dimethoxyethane Chemical compound COCCOC XTHFKEDIFFGKHM-UHFFFAOYSA-N 0.000 description 2
- 241000283086 Equidae Species 0.000 description 2
- QUSNBJAOOMFDIB-UHFFFAOYSA-N Ethylamine Chemical compound CCN QUSNBJAOOMFDIB-UHFFFAOYSA-N 0.000 description 2
- 241000282326 Felis catus Species 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- 241000606766 Haemophilus parainfluenzae Species 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 2
- 239000004472 Lysine Substances 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- CTQNGGLPUBDAKN-UHFFFAOYSA-N O-Xylene Chemical compound CC1=CC=CC=C1C CTQNGGLPUBDAKN-UHFFFAOYSA-N 0.000 description 2
- 102100021079 Ornithine decarboxylase Human genes 0.000 description 2
- 241001494479 Pecora Species 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
- 241000607142 Salmonella Species 0.000 description 2
- 239000002262 Schiff base Substances 0.000 description 2
- 150000004753 Schiff bases Chemical class 0.000 description 2
- 241000191967 Staphylococcus aureus Species 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- WETWJCDKMRHUPV-UHFFFAOYSA-N acetyl chloride Chemical compound CC(Cl)=O WETWJCDKMRHUPV-UHFFFAOYSA-N 0.000 description 2
- 239000012346 acetyl chloride Substances 0.000 description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 2
- 150000000475 acetylene derivatives Chemical class 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 230000001476 alcoholic effect Effects 0.000 description 2
- YIYBQIKDCADOSF-UHFFFAOYSA-N alpha-Butylen-alpha-carbonsaeure Natural products CCC=CC(O)=O YIYBQIKDCADOSF-UHFFFAOYSA-N 0.000 description 2
- 229910021529 ammonia Inorganic materials 0.000 description 2
- 239000003708 ampul Substances 0.000 description 2
- 239000003242 anti bacterial agent Substances 0.000 description 2
- 229940088710 antibiotic agent Drugs 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 239000011668 ascorbic acid Substances 0.000 description 2
- 235000010323 ascorbic acid Nutrition 0.000 description 2
- HUMNYLRZRPPJDN-UHFFFAOYSA-N benzaldehyde Chemical compound O=CC1=CC=CC=C1 HUMNYLRZRPPJDN-UHFFFAOYSA-N 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 150000001780 cephalosporins Chemical class 0.000 description 2
- DCFKHNIGBAHNSS-UHFFFAOYSA-N chloro(triethyl)silane Chemical compound CC[Si](Cl)(CC)CC DCFKHNIGBAHNSS-UHFFFAOYSA-N 0.000 description 2
- MVPPADPHJFYWMZ-UHFFFAOYSA-N chlorobenzene Chemical compound ClC1=CC=CC=C1 MVPPADPHJFYWMZ-UHFFFAOYSA-N 0.000 description 2
- PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical compound NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 description 2
- 230000000593 degrading effect Effects 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000004210 ether based solvent Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- IKDUDTNKRLTJSI-UHFFFAOYSA-N hydrazine monohydrate Substances O.NN IKDUDTNKRLTJSI-UHFFFAOYSA-N 0.000 description 2
- 229930195733 hydrocarbon Natural products 0.000 description 2
- 150000002430 hydrocarbons Chemical class 0.000 description 2
- 239000001257 hydrogen Substances 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 2
- 239000007943 implant Substances 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 230000002427 irreversible effect Effects 0.000 description 2
- 239000013038 irreversible inhibitor Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- ZCSHNCUQKCANBX-UHFFFAOYSA-N lithium diisopropylamide Chemical compound [Li+].CC(C)[N-]C(C)C ZCSHNCUQKCANBX-UHFFFAOYSA-N 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 239000011777 magnesium Substances 0.000 description 2
- 229910052749 magnesium Inorganic materials 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 229910052943 magnesium sulfate Inorganic materials 0.000 description 2
- 235000019341 magnesium sulphate Nutrition 0.000 description 2
- 238000002844 melting Methods 0.000 description 2
- 230000008018 melting Effects 0.000 description 2
- 235000010755 mineral Nutrition 0.000 description 2
- 239000011707 mineral Substances 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
- LQNUZADURLCDLV-UHFFFAOYSA-N nitrobenzene Chemical compound [O-][N+](=O)C1=CC=CC=C1 LQNUZADURLCDLV-UHFFFAOYSA-N 0.000 description 2
- 150000007524 organic acids Chemical class 0.000 description 2
- 150000007530 organic bases Chemical class 0.000 description 2
- 238000007911 parenteral administration Methods 0.000 description 2
- 239000003208 petroleum Substances 0.000 description 2
- HKOOXMFOFWEVGF-UHFFFAOYSA-N phenylhydrazine Chemical compound NNC1=CC=CC=C1 HKOOXMFOFWEVGF-UHFFFAOYSA-N 0.000 description 2
- 229940067157 phenylhydrazine Drugs 0.000 description 2
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 description 2
- 229910052700 potassium Inorganic materials 0.000 description 2
- 239000011591 potassium Substances 0.000 description 2
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 239000002244 precipitate Substances 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- GETQZCLCWQTVFV-UHFFFAOYSA-N trimethylamine Chemical compound CN(C)C GETQZCLCWQTVFV-UHFFFAOYSA-N 0.000 description 2
- 239000008096 xylene Substances 0.000 description 2
- VWVZFHRDLPHBEG-UHFFFAOYSA-N 1-(chloromethyl)-4-methylsulfanylbenzene Chemical group CSC1=CC=C(CCl)C=C1 VWVZFHRDLPHBEG-UHFFFAOYSA-N 0.000 description 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- BVNYROHOUZCIEL-UHFFFAOYSA-N 2,2-diethylbutanal Chemical compound CCC(CC)(CC)C=O BVNYROHOUZCIEL-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- XVMSFILGAMDHEY-UHFFFAOYSA-N 6-(4-aminophenyl)sulfonylpyridin-3-amine Chemical compound C1=CC(N)=CC=C1S(=O)(=O)C1=CC=C(N)C=N1 XVMSFILGAMDHEY-UHFFFAOYSA-N 0.000 description 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- QYPPJABKJHAVHS-UHFFFAOYSA-N Agmatine Natural products NCCCCNC(N)=N QYPPJABKJHAVHS-UHFFFAOYSA-N 0.000 description 1
- 102000004452 Arginase Human genes 0.000 description 1
- 108700024123 Arginases Proteins 0.000 description 1
- 208000024255 Audiogenic seizures Diseases 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 1
- 241000700198 Cavia Species 0.000 description 1
- 241000193455 Clostridium cadaveris Species 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 241000588914 Enterobacter Species 0.000 description 1
- 241000588724 Escherichia coli Species 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- 241000606790 Haemophilus Species 0.000 description 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 1
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical compound ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 description 1
- 241000588748 Klebsiella Species 0.000 description 1
- 201000008225 Klebsiella pneumonia Diseases 0.000 description 1
- 241000588747 Klebsiella pneumoniae Species 0.000 description 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 description 1
- 240000007472 Leucaena leucocephala Species 0.000 description 1
- 235000010643 Leucaena leucocephala Nutrition 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 102000007357 Methionine adenosyltransferase Human genes 0.000 description 1
- 108010007784 Methionine adenosyltransferase Proteins 0.000 description 1
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 description 1
- OPKOKAMJFNKNAS-UHFFFAOYSA-N N-methylethanolamine Chemical compound CNCCO OPKOKAMJFNKNAS-UHFFFAOYSA-N 0.000 description 1
- 102000052812 Ornithine decarboxylases Human genes 0.000 description 1
- 108700005126 Ornithine decarboxylases Proteins 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 208000002606 Paramyxoviridae Infections Diseases 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 206010035717 Pneumonia klebsiella Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 241000193998 Streptococcus pneumoniae Species 0.000 description 1
- 241000193996 Streptococcus pyogenes Species 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 102000003929 Transaminases Human genes 0.000 description 1
- 108090000340 Transaminases Proteins 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- 239000004015 abortifacient agent Substances 0.000 description 1
- 231100000641 abortifacient agent Toxicity 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 150000001242 acetic acid derivatives Chemical class 0.000 description 1
- 125000003668 acetyloxy group Chemical group [H]C([H])([H])C(=O)O[*] 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- QYPPJABKJHAVHS-UHFFFAOYSA-P agmatinium(2+) Chemical compound NC(=[NH2+])NCCCC[NH3+] QYPPJABKJHAVHS-UHFFFAOYSA-P 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001340 alkali metals Chemical class 0.000 description 1
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 1
- 150000001342 alkaline earth metals Chemical class 0.000 description 1
- 125000005103 alkyl silyl group Chemical group 0.000 description 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 description 1
- 239000004411 aluminium Substances 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 235000019270 ammonium chloride Nutrition 0.000 description 1
- 230000003556 anti-epileptic effect Effects 0.000 description 1
- 230000003509 anti-fertility effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 229940072107 ascorbate Drugs 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- TXHIDIHEXDFONW-UHFFFAOYSA-N benzene;propan-2-one Chemical compound CC(C)=O.C1=CC=CC=C1 TXHIDIHEXDFONW-UHFFFAOYSA-N 0.000 description 1
- PASDCCFISLVPSO-UHFFFAOYSA-N benzoyl chloride Chemical compound ClC(=O)C1=CC=CC=C1 PASDCCFISLVPSO-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229920002988 biodegradable polymer Polymers 0.000 description 1
- 239000004621 biodegradable polymer Substances 0.000 description 1
- 230000006696 biosynthetic metabolic pathway Effects 0.000 description 1
- NBLAIKHFQBOVPV-UHFFFAOYSA-N bis(ethoxycarbonyl)azaniumylideneazanide Chemical compound CCOC(=O)[N+](=[N-])C(=O)OCC NBLAIKHFQBOVPV-UHFFFAOYSA-N 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Chemical group 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 235000011089 carbon dioxide Nutrition 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- FUBBGQLTSCSAON-PBFPGSCMSA-N cefaloglycin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)COC(=O)C)C(O)=O)=CC=CC=C1 FUBBGQLTSCSAON-PBFPGSCMSA-N 0.000 description 1
- 229950004030 cefaloglycin Drugs 0.000 description 1
- XIURVHNZVLADCM-IUODEOHRSA-N cefalotin Chemical compound N([C@H]1[C@@H]2N(C1=O)C(=C(CS2)COC(=O)C)C(O)=O)C(=O)CC1=CC=CS1 XIURVHNZVLADCM-IUODEOHRSA-N 0.000 description 1
- 229960000603 cefalotin Drugs 0.000 description 1
- 230000032823 cell division Effects 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- ZAIPMKNFIOOWCQ-UEKVPHQBSA-N cephalexin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)C)C(O)=O)=CC=CC=C1 ZAIPMKNFIOOWCQ-UEKVPHQBSA-N 0.000 description 1
- 229940106164 cephalexin Drugs 0.000 description 1
- 239000003610 charcoal Substances 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- IJOOHPMOJXWVHK-UHFFFAOYSA-N chlorotrimethylsilane Chemical compound C[Si](C)(C)Cl IJOOHPMOJXWVHK-UHFFFAOYSA-N 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 150000001860 citric acid derivatives Chemical class 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- FAMRKDQNMBBFBR-BQYQJAHWSA-N diethyl azodicarboxylate Substances CCOC(=O)\N=N\C(=O)OCC FAMRKDQNMBBFBR-BQYQJAHWSA-N 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 150000002009 diols Chemical class 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 230000013020 embryo development Effects 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- FAMRKDQNMBBFBR-UHFFFAOYSA-N ethyl n-ethoxycarbonyliminocarbamate Chemical compound CCOC(=O)N=NC(=O)OCC FAMRKDQNMBBFBR-UHFFFAOYSA-N 0.000 description 1
- 239000000284 extract Substances 0.000 description 1
- 230000035558 fertility Effects 0.000 description 1
- 210000003754 fetus Anatomy 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 229940050411 fumarate Drugs 0.000 description 1
- 238000007429 general method Methods 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 239000003102 growth factor Substances 0.000 description 1
- 230000009554 growth spurt Effects 0.000 description 1
- 229940093915 gynecological organic acid Drugs 0.000 description 1
- HQLZFBUAULNEGP-UHFFFAOYSA-N hexan-3-amine Chemical compound CCCC(N)CC HQLZFBUAULNEGP-UHFFFAOYSA-N 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 150000007529 inorganic bases Chemical class 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- AFRJJFRNGGLMDW-UHFFFAOYSA-N lithium amide Chemical compound [Li+].[NH2-] AFRJJFRNGGLMDW-UHFFFAOYSA-N 0.000 description 1
- WMWSRIHFAVOHSW-UHFFFAOYSA-N lithium;ethane-1,2-diamine;ethyne Chemical compound [Li+].[C-]#C.NCCN WMWSRIHFAVOHSW-UHFFFAOYSA-N 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- OTCKOJUMXQWKQG-UHFFFAOYSA-L magnesium bromide Chemical compound [Mg+2].[Br-].[Br-] OTCKOJUMXQWKQG-UHFFFAOYSA-L 0.000 description 1
- 229910001623 magnesium bromide Inorganic materials 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 229940049920 malate Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 150000002688 maleic acid derivatives Chemical class 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 150000002739 metals Chemical class 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 229930182817 methionine Natural products 0.000 description 1
- 150000002741 methionine derivatives Chemical class 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000002899 monoamine oxidase inhibitor Substances 0.000 description 1
- SFDZETWZUCDYMD-UHFFFAOYSA-N monosodium acetylide Chemical compound [Na+].[C-]#C SFDZETWZUCDYMD-UHFFFAOYSA-N 0.000 description 1
- HQFYIDOMCULPIW-UHFFFAOYSA-N n-methylprop-2-yn-1-amine Chemical compound CNCC#C HQFYIDOMCULPIW-UHFFFAOYSA-N 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004355 nitrogen functional group Chemical group 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 150000003891 oxalate salts Chemical class 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- QNGNSVIICDLXHT-UHFFFAOYSA-N para-ethylbenzaldehyde Natural products CCC1=CC=C(C=O)C=C1 QNGNSVIICDLXHT-UHFFFAOYSA-N 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 229960004838 phosphoric acid Drugs 0.000 description 1
- NAYYNDKKHOIIOD-UHFFFAOYSA-N phthalamide Chemical compound NC(=O)C1=CC=CC=C1C(N)=O NAYYNDKKHOIIOD-UHFFFAOYSA-N 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000011736 potassium bicarbonate Substances 0.000 description 1
- 235000015497 potassium bicarbonate Nutrition 0.000 description 1
- 229910000028 potassium bicarbonate Inorganic materials 0.000 description 1
- 229910000027 potassium carbonate Inorganic materials 0.000 description 1
- 235000011181 potassium carbonates Nutrition 0.000 description 1
- TYJJADVDDVDEDZ-UHFFFAOYSA-M potassium hydrogencarbonate Chemical compound [K+].OC([O-])=O TYJJADVDDVDEDZ-UHFFFAOYSA-M 0.000 description 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 description 1
- RWMKSKOZLCXHOK-UHFFFAOYSA-M potassium;butanoate Chemical group [K+].CCCC([O-])=O RWMKSKOZLCXHOK-UHFFFAOYSA-M 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 229940116317 potato starch Drugs 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- RZWZRACFZGVKFM-UHFFFAOYSA-N propanoyl chloride Chemical compound CCC(Cl)=O RZWZRACFZGVKFM-UHFFFAOYSA-N 0.000 description 1
- 125000006308 propyl amino group Chemical group 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 229920000260 silastic Polymers 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 229920002379 silicone rubber Polymers 0.000 description 1
- 239000004945 silicone rubber Substances 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- ODZPKZBBUMBTMG-UHFFFAOYSA-N sodium amide Chemical group [NH2-].[Na+] ODZPKZBBUMBTMG-UHFFFAOYSA-N 0.000 description 1
- CDBYLPFSWZWCQE-UHFFFAOYSA-L sodium carbonate Substances [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 230000021595 spermatogenesis Effects 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- IIACRCGMVDHOTQ-UHFFFAOYSA-M sulfamate Chemical compound NS([O-])(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-M 0.000 description 1
- 229940032330 sulfuric acid Drugs 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- RUPAXCPQAAOIPB-UHFFFAOYSA-N tert-butyl formate Chemical group CC(C)(C)OC=O RUPAXCPQAAOIPB-UHFFFAOYSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 238000013519 translation Methods 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Cephalosporin Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
Description
ç£æ¥äžã®å©çšåé
æ¬çºæã¯æ°èŠãªè£œè¬åŠäžæçšãªã¢ãã³ã®ã¢ã»ã
ã¬ã³èªå°äœã«é¢ããã åé¡ã解決ããæ段 æ¬çºæã®ååç©ã¯äžè¬åŒïŒã«ãã€ãŠè¡šãããã ïŒäœãåŒäžïŒ¡ã¯ã¡ãã¬ã³ããšãã¬ã³åã¯ãšããª
ãã³ã§ããïŒã äžè¬åŒïŒã®ååç©ã®è£œè¬åŠçã«åãå ¥ãããã
å¡©åã³åã ã®å åŠç°æ§äœã¯æ¬çºæã®ç¯å²å ã«å«ãŸ
ããã äžã®åŒïŒã«æŒããŠã¡ãã¬ã³ã¯âCH2âã®æå³ã«
çšãããããšãã¬ã³ã¯âCH2CH2âã®æå³ã«çšã
ãããšããªãã³ã¯
ã¬ã³èªå°äœã«é¢ããã åé¡ã解決ããæ段 æ¬çºæã®ååç©ã¯äžè¬åŒïŒã«ãã€ãŠè¡šãããã ïŒäœãåŒäžïŒ¡ã¯ã¡ãã¬ã³ããšãã¬ã³åã¯ãšããª
ãã³ã§ããïŒã äžè¬åŒïŒã®ååç©ã®è£œè¬åŠçã«åãå ¥ãããã
å¡©åã³åã ã®å åŠç°æ§äœã¯æ¬çºæã®ç¯å²å ã«å«ãŸ
ããã äžã®åŒïŒã«æŒããŠã¡ãã¬ã³ã¯âCH2âã®æå³ã«
çšãããããšãã¬ã³ã¯âCH2CH2âã®æå³ã«çšã
ãããšããªãã³ã¯
ãåŒããæå³ããããã«çš
ããããã
äžã®äžè¬åŒïŒããæ¬çºæååç©ã¯ã¢ãã³ã®ã¢ã»
ãã¬ã³èªå°äœã§ããããšãæããã§ããã æ¬çºæååç©ã®è£œè¬åŠçã«åãå ¥ããããå¡©ã®
äŸãæããã°å¡©é žãèåæ°ŽçŽ é žãç¡«é žåã³çé žç
ã®ç¡æ©é žããŸãã¡ã¿ã³ã¹ã«ãã³é žããµãªãã«é žã
ãã¬ã€ã³é žãããã³é žãé ç³é žãã¯ãšã³é žãã¢ã¹
ã³ã«ãã³é žçã®ææ©é žã§åœ¢æãããç¡æ¯æ§é žä»å
å¡©ãåã³ã¢ã«ã«ãªéå±ãäŸãã°ãããªãŠã ãã«ãª
ãŠã ããªããŠã ãã¢ã«ã«ãªåé¡éå±ãäŸãã°ã«ã«
ã·ãŠã åã³ãã°ãã·ãŠã ã第æ軜éå±äŸãã°
ã¢ã«ãããŠã ã第äžçŽã第äºçŽåã¯ç¬¬äžçŽçã®æ
æ©ã¢ãã³é¡äŸãã°ã·ã¯ãããã·ã«ã¢ãã³ããšãã«
ã¢ãã³ãããªãžã³ãã¡ãã«ã¢ãããšã¿ããŒã«ããš
ã¿ããŒã«ã¢ãã³åã³ããã©ãžã³ã®å¡©åºçã®ç¡æ©å
ã¯ææ©å¡©åºã§åœ¢æãããç¡æ¯æ§å¡©ãå«ãŸãããå¡©
ã¯æ £çšã®æ段ã«ãã€ãŠåœ¢æãããã ãã¡ãã¬ã³åã¯ãšããªãã³ã§ããååç©é¡ã
奜ãŸããã¯ããã¡ãã¬ã³ã§ããååç©ã¯ãã奜
ãŸããã æ¬çºæååç©ã®äŸãæããã°ä»¥äžã®éãã§ã
ããïŒæ³šïŒä»¥äžããã¹ã¯ïŒhexïŒã®èš³ã§ãããã
ã»ãšã¯ããªãã€ãã ïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ã ïŒïŒïŒâãããâïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ã ïŒïŒïŒâãããâïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ã æ¬çºæååç©ã®å©çšåé (ã€) äžè¬åŒïŒã®ååç©é¡ã¯ããªã¢ãã³åœ¢æã«ä¿ã
ã«ã«ããã·ã«åºåè§£é µçŽ ã®äžå¯éçé»å®³å€ã§ã
ãè¬çåŠçè©Šè¬ãšããŠãã®ååç©ã¯æçšã§ã
ããããªã¢ãã³ãšãããããã¬ã¹ã·ã³ãã¹ãã«
ããžã³åã³ã¹ãã«ãã³ã¯æ€ç©åã³åç©çµç¹ã«å
åšããŸããã埮çç©äžã«ãååšãããããªã¢ã
ã³é¡ã®æ£ç¢ºãªççåŠç圹å²ã¯æ確ã«ã¯èšè¿°ã¯ãª
ãããããªã¢ãã³ã现èåè£åã³çé·ã«ä¿ãã
ãã€ããšã瀺åãã蚌æ ãããïŒãšã€ã ãžâ
ãŠã€ãªã¢ã ãºâã¢ã·ãŠãã³çïŒH.G.
WilliamsâAshman et alïŒãThe ltalian J.
Biochem.25ïŒïŒâ32ïŒ1976ïŒããšã€ã©ã€ã ã¢
ã³ã ãžãšãŒ ãžãšãŒã³ïŒA.Raina and J.
JanneïŒãMed.Biol.53ïŒ121â147ïŒ1975ïŒåã³
ãã€ãŒ ãšã€ã ã©ãã»ã«ïŒD.H.RussellïŒã
Life Science 13ïŒ1635â1647ïŒ1973ïŒãããªã¢
ãã³ã¯äŸãã°ã€ãŒ ã³ãªïŒE.coliïŒããšã³ãã
ãã¯ã¿ãŒïŒEnterobacterïŒãã¯ã¬ãã·ãšã©
ïŒKlebsiellaïŒãã¹ã¿ãã€ãã³ãã«ã¹ãªãŒã¬ãŠã¹
ïŒStaphylococcus aureusïŒãã·ãŒ ã«ãããªã¹
ïŒC.cadaverisïŒããµã«ã¢ãã©ã¯ã¿ã€ããªãµ
ïŒSalmonella typhosaïŒåã³ããšã¢ãã€ã©ã¹ã
ã©ã€ã³ãã«ãšã³ã¶ïŒHaemophilus
parainfluenzaïŒãªã©ããçš®ã®åŸ®çç©ã«å¯Ÿãã
å¿ é çé·å åã§ãããåã¯çé·éçšã«ä¿ããæ
ãããããªã¢ãã³ã¯çŽ°èå¢æ®ãèµ·ããåºæ¿ã«ç¶
ããŠåæåã³èç©ã®å¢å ãããã®ã§æ£åžžãªçé·
åã³æ°çç©ã®æ¥çé·ã®äž¡æ¹å ±ã«é¢ä¿ãããããŸ
ããããªã¢ãã³æ°Žæºã¯èçµç¹ãçœè¡ç 现èåã³
ä»ã®æ¥æé·çµç¹ã«æŒããŠé«ãããšãç¥ãããŠã
ãããªã«ããã³ãâã¢ããã·ã«ã¡ããªãã³ã
ã¢ã«ã®ãã³åã³ãªãžã³ã®ã«ã«ããã·ã«åºåè§£é µ
çŽ ã®æŽ»æ§ãšããªã¢ãã³åœ¢æãšã®éã«çžé¢é¢ä¿ã
ããããšãç¥ãããŠããã ããã¬ã·ã³ãã¹ãã«ããžã³åã³ã¹ãã«ãã³ã®
çåæã¯çžäºã«é¢ä¿ããŠãããããã¬ã·ã³ã¯ãª
ã«ããã³ã«ã«ããã·ã«åºåè§£é µçŽ ã«ãã觊åªã
ãããªã«ããã³ã®è±ã«ã«ããã·ã«åïŒè±çé žïŒ
çæç©ã§ãããããã¬ã·ã³çæã¯ãŸãã¢ã«ã®ã
ã³ãè±çé žãããŠã¢ã°ããã³ãçãããããå
æ°Žå解ãããŠããã¬ã·ã³ãšå°¿çŽ ãçæããããš
ã«ãã€ãŠãçãåŸããã¢ã«ã®ãã³ããŸãé µçŽ ã¢
ã«ã®ããŒãŒã®äœçšã«ãã€ãŠãªã«ããã³åœ¢æã«ä¿
ã€ãŠããããšã¹âã¢ããã·ã«ã¡ããªãã³ã·ã³ã»
ã¿ãŒãŒã«ããã¡ããªãã³ã®æŽ»æ§åãâã¢ãã
ã·ã«ã¡ããªãã³ã圢æããããã¯è±çé žããã
ãããã®ã¡ã«æŽ»æ§åãããã¡ããªãã³ã®ããã
ã«ã¢ãã³éšåãããã¬ã·ã³ã«ç§»ãããããšãåº
æ¥ãã¹ãã«ããžã³ã圢æããã¹ãã«ããžã³ãã¹
ãã«ãã³ã圢æãããåŸã€ãŠããã¬ã·ã³ãã¹ã
ã«ããžã³åã³ã¹ãã«ãã³ã®åé§äœãšããŠåãã
æŽã«ãããã¬ã·ã³ã®åæå¢å ã¯çµç¹ãæ¹æ°ãã
ãçé·éçšãåããæåã®åŸŽåã§ããããšã瀺
ãããŠãããšããç¹ã«æŒããŠããããããªã¢ã
ã³çåæçµè·¯ã®é¡èãªå¶åŸ¡å¹æãæããããšã
瀺ããŠããããªãžã³ã®è±çé žçæç©ã§ããã«ã
ããªã³ã¯ïŒ³âã¢ããã·ã«âã¡ããªãã³ã«ã«ãã
ã·ã«åºåè§£é µçŽ ã®æŽ»æ§ãåºæ¿ããããšã瀺ãã
ãŠããããŸãå€ãã®åŸ®çç©ãäŸãã°ãšã€ã ã
ã©ã€ã³ãã«ãšã³ã¶ïŒH.parainfluenzaïŒã®çé·
éçšã«å¿ é ã§ããããšãç¥ãããŠããã (ã) åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšããªãã³ã§
ããååç©ã¯ããçš®ã®æ¥æé·éçšãæå¶ããã®
ã«ãæçšã§ãããäŸãã°è©²ååç©ã¯ç²Ÿå圢æå
ã³è圢æã®é»å®³ã«æçšã§ãããåŸã€ãŠéã®å粟
é»æ¢å€åã³å èè¬ãšããŠã®çšéãèŠåºããŠã
ãããã®ååç©ã¯ãŸãæ°çç©çé·äŸãã°å å®æ§
è «çãçœè¡ç ããªã³ãè «ã®æå¶ã«æçšã§ããã
äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšãã¬ã³ã§
ããååç©ãæäžããã«æŒããŠã¯ãåæã«æ¢ç¥
ã®æé ã«ãã€ãŠãã©ã³ã¹ïŒÂ±ïŒâïŒâããšãã«
ã·ã¯ããããããã³ïŒtransïŒÂ±ïŒâïŒâphenyl
âcycloproponamineïŒåã¯ïŒ®âãã³ãžã«â
âã¡ãã«âïŒâããããã«ã¢ãã³çã®ã¢ãã¢ã
ã³ãªãã·ããŒãŒé»å®³å€ãæäžããã®ãæãŸãã
ãããããªããäžè¬åŒïŒååç©ã®ãªã«ããã³å
ã¯ïŒ³âã¢ããã·ã«ã¡ããªãã³ã«ã«ããã·ã«åºå
è§£é µçŽ ã®äžå¯éçé»å®³å€ãšããŠã®æçšæ§ã¯æ¬¡ã®
æ§ã«ããŠæž¬å®ã§ãããé©åœãªååç©ã®æ°Žæº¶æ¶²ã
çµå£çåã¯éçµå£çã«éã©ããåã¯ããŠã¹ã«äž
ãããããååç©æäžåŸïŒä¹è³48æéåŸã«åç©
ã殺ãåç«è ºã®è ¹åŽèãé€å»ããå質åãããª
ã«ããã³åã³ïŒ³âã¢ããã·ã«ã¡ããªãã³ã«ã«ã
ãã·ã«åºåè§£é µçŽ æŽ»æ§ãã€ãŒ ãšãŒ ããã°
ïŒE.A.PeggïŒåã³ãšã€ã ãžãŒ ãŠã€ãªã¢ã ã¹
âã¢ãã·ãŠãã³ïŒH.G.WilliamsâAshmanïŒã
Biochem.J.108ïŒ533â539ïŒ1968ïŒåã³ãžãšãŒ
ãžãšãŒã³ïŒJ.JanneïŒåã³ãšã€ã ãžãŒ ãŠ
ã€ãªã¢ã ã¹âã¢ãã·ãŠãã³ãBiochem.and
Biophys.Res.Comm.42 222â228ïŒ1971ïŒã«æŠ
ç¥çã«èšèŒãããæ§ã«æž¬å®ãããã (ã) äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšãã¬ã³
ã§ããååç©ã¯æ¬¡ã®æ§é ïŒåŒäžïŒã¯ïŒåã¯ïŒïŒãæããååç©ã®ä»£è¬
åé§äœã§ãããåŒïŒã®ååç©ã¯Î³âã¢ããé ªé ž
ãã©ã³ã¹ã¢ãããŒãŒã®äžå¯éçé»å®³å€ãšããŠç¥
ãããæäžã«ãã€ãŠÎ³âã¢ããé ªé žïŒGABAïŒ
ã®é«ãè³å æ°Žæºãçããã (ã) äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšãã¬ã³
ã§ããååç©ã¯åŒïŒã®ååç©ã«ä»£è¬çã«å€æã§
ããããšã¯ãçŸåšæãŠããã掻æ§ãç«èšŒããã®
ã«çšããããŠããã·ã ã©ãŒïŒSimlerïŒçã
Biochem.Pharmacol.22ïŒ1701ïŒ1973ïŒã«ãã
èšèŒãããäžè¬æ¹æ³ã«ãã€ãŠæž¬å®ãããDBA
系統ã®ããŠã¹ã®èŽåæ§ã®æ¥çºäœã«å¯Ÿãããã®å
åç©ã®ä¿è·äœçšã«ãã€ãŠäŸç€ºãããããšãåºæ¥
ãã ããã (ã) äžè¬åŒïŒã®ååç©ã¯æ¬¡ã®äžè¬åŒïŒã®æ°èŠãªã»
ãã¢ãã¹ããªã³èªå°äœã®è£œé ã®ååŠäžéäœç©è³ª
ãšããŠæçšã§ãããåŒïŒã®ã»ãã¢ãã¹ããªã³å
åç©ã¯æçç©è³ªãšããŠæçšã§ããã äžã®äžè¬åŒïŒã«æŒããŠïŒ¡ã¯äžè¬åŒïŒã§ã®å®çŸ©
ãšåãæå³ãæã¡ãïŒã¯æ°ŽçŽ åã¯è² é»è·ããŸã
ã¯æ°ŽçŽ åã¯ã¢ã»ããã·ã§ããã äžè¬åŒïŒã®ååç©åã³ãããã®è£œè¬åŠçã«å
ãå ¥ããããå¡©åã³åã ã®å åŠç°æ§äœã¯æçç©
質ãšããŠæçšãªæ°èŠãªååç©ã§ãã€ãŠå€ãã®è¯
ãç¥ãããã»ãã¢ãã¹ããªã³èªå°äœäŸãã°ã»ã
ã¢ã¬ãã·ã³ãã»ãã¢ããã³ãåã¯ã»ãã¢ãã°ãª
ã·ã³ãšåæ§ã®æ¹æ³ã§æäžãããããšãåºæ¥ãã
äžè¬åŒïŒã®ååç©åã³ãããã®è£œè¬åŠçã«åã
ãããããå¡©åã³ç°æ§äœé¡ã¯åç¬ã§åã¯è£œè¬åŠ
çåŠæ¹å€ãšããŠçµå£çåã¯éçµå£çåã³å±æç
ã«æž©è¡åç©å³ã¡é³¥åã³åºä¹³é¡ãäŸãã°ç«ãç¬ã
çãçŸã銬åã³äººéã«æäžãããããšãåºæ¥
ããçµå£æäžãšããŠã¯æ¬ååç©ã¯é å€ãã«ãã»
ã«å€ãåã¯äžžè¬ã®åœ¢ã§åã¯ãšã«ããžãŒã«åã¯æž
æ¿å€ã®åœ¢ã§æäžãããããéçµå£æäžã«ã¯ãæ¬
ååç©ã¯ä»ã®æº¶è³ªäŸãã°æº¶æ¶²ãç匵ã«ãããã
ã®å åãªå¡©æ°Žåã¯ã°ã«ã³ãŒã¹ãå«ã¿ããæ» èæ°Ž
溶液ã®åœ¢ã§äœ¿çšãããã®ãæãè¯ãã§ãããã
å±ææäžã«ã¯ãäžè¬åŒïŒã®ååç©åã³ãããã®
å¡©åã³ç°æ§äœé¡ã¯ã¯ãªãŒã åã¯è»èäžã«æ··å ¥ã
ããã äžè¬åŒïŒã®ååç©åã³ãããã®è£œè¬åŠçã«å
ãå ¥ããããå¡©é Œåã³åã ã®å åŠç°æ§äœé¡ã察
æãã掻æ§ãæãã埮çç©ã®äŸãæããã°ãã¹
ã¿ãã€ãã³ãã«ã¹ ãªãŒã¬ãŠã¹
ïŒStaphylococcus aureusïŒããµã«ã¢ãã© ã·ãš
ããã ãšã¬ãªïŒSalmonella schotmuehleriïŒã
ã¯ã¬ãã·ãšã© ããŠãŒã¢ãã¢ïŒKlebsiella
pneumoniaeïŒããã€ããã³ãã«ã¹ ããŠãŒã¢
ãã¢ãšïŒDiplococcus pneumoniaeïŒåã³ã¹ã
ã¬ããã³ãã«ã¹ ããªã²ãã¹ïŒStreptococcus
pyogenesïŒã§ããã äžè¬åŒïŒã®ååç©ã®è£œè¬åŠçã«åãå ¥ããã
ãç¡æ¯æ§ã®ç¡æ©é žä»å å¡©ãäŸç€ºããã°ãé±é žä»
å å¡©äŸãã°å¡©é žãèåæ°ŽçŽ é žå¡©ãç¡«é žå¡©ãã¹ã«
ãã¢ãã³é žå¡©ãçé žå¡©åã³ææ©é žä»å å¡©äŸãã°
ãã¬ã€ã³é žå¡©ãé ¢é žå¡©ãã¯ãšã³é žå¡©ãä¿®é žå¡©ã
ãã¯ãé žå¡©ãå®èéŠé žå¡©ãé ç³é žå¡©ããããŒã«
é žå¡©ãææªé žå¡©åã³ã¢ã¹ã³ã«ãã³é žå¡©ã§ããã
å¡©é¡ã¯æ £çšã®æ段ã«ãã€ãŠã€ããããšãåºæ¥
ãã äžè¬åŒïŒã®ååç©ã®äŸãæããã°ïŒæ¬æ现æž
äžãã³ãã¯ïŒpentïŒãããã¯ïŒbutïŒããªã¯ãã¯
ïŒoctïŒã®èš³ã§ãããïŒ ïŒâïŒâïŒâïŒïŒâã¢ã»ãã¬ã³âïŒâã¢ã
ãããâïŒâãšãã«ã¢ããã¡ãã«ïŒããšãã«ïŒœ
ã¢ã»ãã«ïŒœã¢ããâïŒâã¢ã»ãããã·ã¡ãã«
âïŒâãªããœâïŒâãã¢âïŒâã¢ã¶ãã·ã¯ã
ïŒïŒïŒïŒïŒïŒœãªã¯ãâïŒâãšã³âïŒâã«ã«ã
ã³é žã§ããã æäžæ¹æ³ïŒœ è¬çåŠçã«æçšãªè¬å€ãšããŠäžè¬åŒïŒã®ååç©
ã¯ææã®å¹æãéæããããã«æ²»çãããæ£è ã«
çš®ã ã®æ¹æ³ã§æäžãããããè¬çåŠçã«æçšãªæ¬
çºæååç©ã¯åç¬ã§åã¯ä»ãšã®çµã¿åããã§äœ¿çš
ããããããŸããæ¬çºæã®è¬çåŠçã«æçšãªåå
ç©ã¯ã補è¬åŠçãªåŠæ¹å€ã®åœ¢ã§æäžãããŠãè¯
ããååç©ã¯çµå£çã«ãéçµå£çã«ãäŸãã°éè
å ãè ¹è å åã¯ç®äžã«ãããåã¯å±æçã«æäžã
ããããæäžãããååç©ã®éã¯åºãç¯å²ã«ãã€
ããŠå€ããã§ãããããä»»æã®æå¹éã§ããã
ããæ²»çãããæ£è ãæ²»çãã¹ãçç¶ãåã³æäž
æ¹æ³ã«äŸåããŠãååç©ã®æå¹éã¯åäœé©éåœã
æ£è ã®äœéããã°ã©ã åœãçŽ0.1mgä¹è³500mgã§å€
åãã奜ãŸããã¯åäœé©éåœãæ£è ã®äœéããã°
ã©ã åœãçŽ10mgä¹è³çŽ100mgã奜ãŸããã§ãããã
äŸãã°å žåçãªåäœæäžåœ¢åŒã¯åŒïŒã®ååç©10ä¹
è³300mgãå«ãé å€ã§ãã€ãŠææã®å¹æãéæã
ãããã«ã¯æ²»çãããæ£è ã«ïŒæ¥ïŒä¹è³ïŒåæäž
ãããããšãåºæ¥ããããã«äœ¿çšãããæ£è ã®çš
èªã¯åºä¹³é¡äŸãã°ç«ãç¬ãã©ãããããŠã¹ãã¢ã«
ã¢ããã銬ãçãçŸåã³äººéçã®æž©è¡åç©ãæå³
ããæ§ã«äœ¿çšãããã åºäœã®é©éåäœåœ¢åŒã¯æ £çšã®ãã®ã§ããããšã
åºæ¥ããåºäœåœ¢åŒã¯æ¬çºææ°èŠååç©ãšæ äœäŸã
ã°æ»å€åã³ä¹³ç³ãã·ãšç³åã³ã³ãŒã³ã¹ã¿ãŒãçã®
äžæŽ»æ§ã®å å¡«å€ãå«ãã æ®éã®ãŒã©ãã³åã®ãã®
ã§ããããã»ãã»ã«å€ã§ããããšãåºæ¥ããå¥ã®
å ·äœäŸã§ã¯æ°èŠååç©ã¯ä¹³ç³ãã·ãšç³åã¯ã³ãŒã³
ã¹ã¿ãŒãçã®éåžžã®é å€ããŒã¹ãšã¢ã«ã·ã¢ãã³ãŒ
ã³ã¹ã¿ãŒãåã¯ãŒã©ãã³çã®çµåå€ãã³ãŒã³ã¹ã¿
ãŒãããžã€ã¬ã€ã¢æŸ±ç²ãåã¯ã¢ã«ã®ã³é žçã®åŽ©å£
å€åã³ã¹ãã¢ãªã³é žåã¯ã¹ãã¢ãªã³é žãã°ãã·ãŠ
ã çã®æ»å€ãšã®çµã¿åããã§é å€åãããã éçµå£æäžã«ã¯ãæ¬ååç©ã¯ççåŠçã«èªãã
ãåžéå€äžã®æ¬ååç©ã®æº¶æ¶²åã¯æžæ¿æ¶²ã®ãè¡šé¢
掻æ§å€åã³ä»ã®è£œè¬äžèªãããäœè¬ãæ·»å ããå
ã¯æ·»å ããªãæ°Žåã¯æ²¹çã®æ» è液äœã§ãããã補
è¬åŠçæ äœãå«ãã 泚å°å¯èœãªé©é圢åŒãšããŠæ
äžããããããããã®åŠæ¹å€äžã«çšãããããæ²¹
ãäŸç€ºããã°ãç³æ²¹ãåç©ãæ€ç©åã¯åæèµ·æºã®
ãã®äŸãã°ããŒãããæ²¹ã倧è±æ²¹åã³é±æ²¹ã®ãã®
ã§ãããäžè¬ã«ãæ°Žãå¡©æ°Žãæ°Žæ§ããã¹ãããŒã¹
åã³é¢é£ããç ç³æº¶æ¶²ããšã¿ããŒã«åã³ãããã¬
ã³ã°ãªã³ãŒã«åã¯ããªãšãã¬ã³ã°ãªã³ãŒã«ãªã©ã®
ã°ãªã³ãŒã«é¡ã¯å¥œãŸãã液äœæ äœã§ããç¹ã«æ³šå°
å¯èœæº¶æ¶²ã«ã¯å¥œãŸããã æ¬ååç©ã¯æŽ»æ§æåã®æç¶æ§æŸåºãå¯èœã«ãã
æ§ãªæ¹æ³ã§åŠæ¹ãããã貯èµæ³šå°ïŒdepot
injectionïŒåã¯æ¿å ¥åŠæ¹å€ã®åœ¢åŒã§æäžããã
ããšãåºæ¥ãã掻æ§æåã¯ãã¬ããåã¯å°ããªç
ã«å§çž®ããç®äžã«åã¯çèå ã«è²¯èµæ³šå°åã¯ã€ã³
ãã©ã³ããšããŠæ¿å ¥ããããã€ã³ãã©ã³ãã¯çç©
å解å¯èœãªéåäœåã¯åæã·ãªã³ã³é¡äŸãã°ããŠ
ã³ãŒãã³ã°ç€Ÿã«ãã補é ãããã·ãªã³ã³ãŽã ã®ã·
ã©ã¹ãã€ãã¯ïŒSilasticïŒãªã©ã®äžæŽ»æ§ç©è³ªãçš
ããããšãåºæ¥ãã 補æ³ïŒœ äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšããªãã³
ã§ããååç©ã¯ãä»»æã«ïŒäŸ¡ã®éå±ã«ããªã³äŸã
ã°ãšãŠåäºéãåã¯èåãã°ãã·ãŠã ã®ååšã®äž
ã«ãïŒåœéã®é©åœã«ä¿è·ããããããã«ã®ã«ã¢ã
ã³ã匷塩åºã§åŠçããŠãä¿è·ããããããã«ã®ã«
ã¢ãã³ãã«ã«ãããªã³äžéäœãçæãããããïŒ
âãããããŒã«åã¯ããããŒã«ã§ã¢ã«ãã«åããŠ
ããã²ã³åã¢ã«ã«ãã€ã«äŸãã°å¡©åã¢ã»ãã«åã¯
å¡©åããããªãã«ãåã¯å¡©åãã³ãŸã€ã«ã®æ§ãªã
ãã²ã³åã¢ããŒã€ã«ãåã¯äœçŽã¢ã«ãã«ããããŒ
ã¡ãŒãçã®é žããã²ã³åç©åã¯ç¬¬ïŒçŽãããã·ã«
ã«ããã«ã¢ãžãã§ã¢ã·ã«åããç¶ãã§ïŒâã¢ãã
âïŒâããªã¡ãã«ã·ãªã«ã¢ã»ãã¬ã³ããâïŒâãš
ã³âïŒâãªãŒã«ã®ã¢ããåã¯ã«ã«ãã¡ãŒãã«å æ°Ž
å解ãããããéçé žãããªãŠã åã¯éçé žã«ãª
ãŠã ãçé žãããªãŠã åã¯çé žã«ãªãŠã ãæ°Žé žå
ãããªãŠã åã¯æ°Žé žåã«ãªãŠã çã®å¡©åºã§åŠçã
ãŠïŒâã¢ããããã¹âïŒâãšã³âïŒâã€ã³âïŒâ
ãªãŒã«ã®ã«ã«ããã·ã¢ãããåŸãããã溶åªäŸã
ã°ãžãšãã«ãšãŒãã«ãããã©ããããã©ã³ããžãª
ããµã³ããžã¡ããã·ãšã¿ã³ãªã©ã®ãšãŒãã«é¡ãã
ã³ãŒã³åã¯ãã«ãšã³ãªã©ã®çåæ°ŽçŽ äžã§æ°ŽçŽ åã
ããªãŠã ãã«ãªãŠã 第ïŒãããã·ãããªããŠã ã¢
ã«ãã«ã¢ããäŸãã°ãªããŠã ãžã€ãœãããã«åã¯
ã¢ã«ãã«ãªããŠã ãªã©ã®è§Šåªéã®å¡©åºã®ååšäž
ã«ãçŽâ30ããïŒâã«æŒããŠçŽ30åãïŒæéããª
ã¯ããã¢ã»ããããªã«ã§åŠçããããšã«ãããã
ãªã¯ããã¡ãã«ã€ãããŒããšã¹ãã«ãåŸãããã
çŽ110ãã140âã«æŒããŠé極æ§æº¶åªäŸãã°ãã·ã¬
ã³ããã«ãšã³ãããããã³ãŒã³åã¯ã¯ãããã³ãŒ
ã³äžã§çŽïŒã10æéå ç±ããŠããªã¯ããã¡ãã«ã¢
ã»ãã¢ãããåŸããããé žæ°Žæº¶æ¶²äŸãã°å¡©é žåã¯
å¡©åºæ°Žæº¶æ¶²äŸãã°æ°Žé žåãããªãŠã åã¯æ°Žé žåã«
ãªãŠã ãçšããŠå æ°Žå解ããããšã«ãã€ãŠè£œé ã
ããã äžè¿°ã®ã¢ã«ãã«ååã¯ã¢ã·ã«ååå¿ã¯äžæ§æº¶åª
äŸãã°ãã³ãŒã³ããã«ãšã³ããšãŒãã«ãããã©ã
ãããã©ã³ããžã¡ãã«ã¹ã«ããã·ãåã¯ãããµã¡
ãã«ãã¹ãã«ããªã¢ããäžã§è¡ããããåå¿æž©åºŠ
ã¯â125ãä¹è³25âã§çŽ30åã24æéã®éã§å€åã
ããã ïŒâã¢ããâïŒâããªã¡ãã«ã·ãªã«ã¢ã»ãã¬ã³
ããâïŒâãšã³âïŒâãªãŒã«ã®ã¢ãããåŸããã
ã®å æ°Žå解ã¯ããã©ãžã³ãããšãã«ããã©ãžã³å
ã¯ããããã·ã«ã¢ãã³ã§åŠçããããšã«ããåã¯
é±é žäŸãã°å¡©é žã§åŠçããŠç¶ããŠããªã¡ãã«ã¢ã
ã³åã¯ããªãžã³çã®ææ©å¡©åºã§ã¡ã¿ããŒã«åã¯ãš
ã¿ããŒã«çã®äœçŽã¢ã«ã³ãŒã«æ§æº¶åªäžã«æŒããŠçŽ
80ã110âã§30åãïŒæéåŠçããããšã«ããé
æãããã äžã®åå¿ã§çšããããé©åœã«ä¿è·ãããããã
ã®ã«ã¢ãã³ã¯æ¬¡ã®äžè¬åŒïŒã§è¡šããããã åŒäžR8ã¯ççŽ ååïŒãïŒåãæããçŽéåã¯
åå²éã¢ã«ãã«ãäŸãã°ã¡ãã«ããšãã«ãïœâã
ããã«åã³ç¬¬äžâããã«åã¯ããªãšãã«ã¡ãã«ã§
ãããåŒïŒã®ååç©ã¯ãããã®ã«ã¢ãã³ã®ã¢ã»ã
ã¬ã³åºåã³çªçŽ å®èœåºäžã«ä¿è·åºãä»å ããŠè£œé
ãããããããã®ã«ã¢ãã³ã®çªçŽ å®èœåºã®ä¿è·ã¯
æ¢ç¥ã®æ¹æ³ã«ãããã³ãºã¢ã«ããããïŒïŒïŒâãž
ã¡ãã«ãããããŒã«åã³ïŒïŒïŒâãžãšãã«ãã¿ã
ãŒã«ããéžã°ããéãšããŒã«ååã«ã«ããã«å«æ
ååç©ã§ã·ããå¡©åºã圢æããŠè¡ãªããããã¢ã»
ãã¬ã³å®èœåºã®ä¿è·ã¯äžè¿°ã®ã·ããå¡©åºãã¢ã«ã
ã«éšåãççŽ ååïŒãïŒåãæãçŽéåã¯åå²é
ã®ããªã¢ã«ãã«ã·ãªã«ã¯ãã©ã€ãäŸãã°ããªã¡ã
ã«ã·ãªã«ã¯ãã©ã€ãåã¯ããªãšãã«ã·ãªã«ã¯ãã©
ã€ããšåå¿ããæ¢ç¥ã®æ¹æ³ã«ãã察å¿ããããªã¢
ã«ãã«ã·ãªã«èªå°äœã圢æããããšã«ããéæã
ããã ã«ã«ãããªã³ã圢æããããã«äžã®åå¿ã§çšã
ãããé©åœãªåŒ·å¡©åºã¯ã¢ã«ãã«ãªããŠã äŸãã°ã
ãã«ãªããŠã ãåã¯ããšãã«ãªããŠã ããªããŠã
ãžã¢ã«ãã«ã¢ããäŸãã°ãªããŠã ãžã€ãœãããã«
ã¢ããããªããŠã ã¢ããã第ïŒçŽã«ãªãŠã ããã¬
ãŒãåã¯ãããªãŠã ã¢ããçã®ã¢ã»ãã¬ã³éšåã«
é£æ¥ããççŽ ååãããããã³ãæãåããã®ã§
ããã äžè¬åŒïŒã«æŒããŠãããšãã¬ã³ã§ããååç©
ã¯ïŒâããããã·ãã³ãâïŒâãšããŒã«ãåŒ
HCCMâ²ïŒåŒäžMâ²ã¯ãããªãŠã ããªããŠã åã¯
MgXâ²ã§ãããããã§Xâ²ã¯å¡©çŽ åã¯èçŽ ã§ããïŒ
ã®éå±ã¢ã»ããªãã§åã¯æ¶²äœã¢ã³ã¢ãã¢ããžã¡ã
ã«ã¹ã«ããã·ãããšãŒãã«é¡äŸãã°ããã©ããã
ãã©ã³ããžãªããµã³ããžãšãã«ãšãŒãã«åã¯ãžã¡
ããã·ãšã¿ã³ãªã©ã®æº¶åªäžã®ãªããŠã ã¢ã»ããª
ãïŒãšãã¬ã³ãžã¢ãã³ã®é¯äœã§çŽâ30ãã25âã«
æŒããŠçŽïŒåãïŒæéåŠçããŠãããâïŒâãšã³
âïŒâã€ã³âïŒïŒïŒâãžãªãŒã«ãåŸãããšã«ãã
補é ãããããããªãŠã åã¯ãªããŠã ã¢ã»ããªã
ãçšãããããšãã«ã¯æ¶²äœã¢ã³ã¢ãã¢ã奜ãŸãã
溶åªã§ããããªããŠã ã¢ã»ããªããçšãããããš
ãã¯ãšãŒãã«æº¶åªã奜ãŸããããšãŒãã«æº¶åªã¯å¥œ
ãŸããåå¿æž©åºŠçŽïŒã25âã§ããã²ã³åãã°ãã·
ãŠã ãçšãããããšãã«å¥œãŸããããªããŠã ã¢ã»
ããªãâãšãã¬ã³ãžã¢ãã³é¯äœãçšãããããšã
ã«ã¯ã枩床25âãæéçŽïŒã12æéãçšããŠå¥œãŸ
ãã溶åªããžã¡ãã«ã¹ã«ãããµã€ãã§ããã ãžãªãŒã«èªå°äœã¯ãã¿ã©ãããããªããšãã«ã
ã¹ãã€ã³åã³ãžãšãã«ãžã¢ãŸãžã«ã«ããã·ã¬ãŒã
ã§ããã©ããããã©ã³ããžãšãã«ãšãŒãã«åã¯ãž
ãªããµã³ãªã©ã®ãšãŒãã«äžã«æŒããŠçŽïŒã12æé
çŽ25ãã50âã§åŠçããã察å¿ãããžãã¿ã«ã¢ã
ãèªå°äœãäžããããã¯ã¡ã¿ããŒã«åã¯ãšã¿ããŒ
ã«ãªã©ã®äœçŽã¢ã«ã³ãŒã«æº¶åªäžã§ããã©ãžã³æ°Žå
ç©ã«ããçŽïŒãïŒæéçŽ25ãã50âã§åŠçããã
次ãã§é žäŸãã°6N HClã§100âãïŒã10æéåŠ
çãããã åèäŸ ïŒäžéäœãšããŠã®çšéïŒ ïŒâïŒâïŒâïŒïŒâã¢ã»ãã¬ã³âïŒâã¢ãã
ãã³ãâïŒâãšãã«ã¢ããã¡ãã«ïŒããšãã«ïŒœ
âã¢ã»ãã«ïŒœã¢ããâïŒâã¢ã»ãããã·ã¡ã
ã«âïŒâãªããœâïŒâããªâïŒâã¢ã¶ãã·ã¯ã
âïŒïŒïŒïŒïŒïŒœãªã¯ãâïŒâãšã³âïŒâã«ã«
ãã³é ž 50mlã®ãšã¿ããŒã«äžã®ïŒïœã®ïŒâã¢ã»ãããã·
ã¡ãã«âïŒâïŒâïŒâã¯ããã¡ãã«ïŒããšã
ã«ïŒœã¢ã»ãã«ïŒœã¢ããâïŒâãªããœâïŒâãã¢
âïŒâã¢ã¶ãã·ã¯ãïŒïŒïŒïŒïŒïŒœâãªã¯ãâïŒ
âãšã³âïŒâã«ã«ãã³é žåã³ã¢ã»ãã¬ã³å®èœåºã«
察ããŠæ«ç«¯ã®ã¢ããåºããã¿ã«ã€ãããšããŠä¿è·
ãããŠããïŒïœã®ïŒïŒïŒâãããâïŒâãšã³âïŒ
âã€ã³ãžã¢ããã®æ··åç©ã25âã§24æéæ¹æããŠ
ãã溶åªãé€å»ããŠæ®æž£ãæ®ãããããããã©ãž
ã³ã§åŠçããŠæº¶åºæ¶²ãšããŠãã³ãŒã³âã¢ã»ãã³ã
çšããŠã·ãªã«ã²ã«äžã§ã¯ãããã°ã©ãã«ããïŒâ
ïŒâïŒâïŒâã¢ã»ãã¬ã³âïŒâã¢ãããã³ã
âïŒâãšãã«ã¢ã»ãã«ïŒœã¢ããâïŒâã¢ã»ãã
ãã·ã¡ãã«âïŒâãªããœâïŒâãã¢âïŒâã¢ãµã
ã·ã¯ãâïŒïŒïŒïŒïŒïŒœãªã¯ãâïŒâãšã³âïŒâ
ã«ã«ãã³é žãåŸãã 以äžã«äžè¬åŒïŒã®ååç©ã®è£œè¬åŠçåŠæ¹å€ãäŸ
瀺ããã 硬質ãŒã©ãã³ã«ãã»ã«ã®çµæã¯ä»¥äžã®æ§ã«äŸç€º
ãããã (a) ïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ 20mg (b) æ»ç³ ïŒmg (c) ä¹³ç³ 90mg åŠæ¹å€ã¯(a)ãš(b)ã®ä¹Ÿç¥ç²æ«ã现ã¡ãã·ãŠã®ç¯©ã«
éããããããååæ··åããããšã«ãã€ãŠé ãã
ããç²æ«ã¯æ¬¡ã«ç¡¬è³ªãŒã©ãã³ã«ãã»ã«ã«æ£å³å å¡«
éã«ãã»ã«åœã115mgã§ã€ããããã 泚å°çšæžæ¿æ¶²çšã®çµæãäŸç€ºãããã®ã¯ä»¥äžã®
çèå 泚å°çšã®ïŒmlã®ã¢ã³ãã«ã§ããã ééããŒã»ã³ã (a) ïŒïŒïŒâãããâïŒâãšã³â âïŒâã€ã³ãžã¢ãã³ 1.0 (b) ããªããã«ãããªãã³ 0.5 (c) ã¬ã·ãã³ 0.25 (d) 100ã«ãã泚å°çšæ°Ž (a)ãš(b)ã®ç©è³ªãæ··åããå質ã«ãããŠïŒmlã®ã¢
ã³ãã«ã«å å¡«ãããããã·ãŒã«ããŠ20åé121â
ã§ãªãŒãã¯ã¬ãŒãã«ããããåã¢ã³ãã«ã¯mlåœã
æ°èŠååç©(a)10mgãå«ãã 次ã®å®æœäŸã¯æ¬çºæã®ååç©ãæŽã«äŸç€ºããã å®æœäŸ ïŒ ïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãžã¢ãã³
ãžãããã¯ãã©ã€ã 500mlã®ããã©ããããã©ã³äžã®21.5ïœ
ïŒ0.1MïŒã®ïŒâããªã¡ãã«ã·ãªã«ãããâïŒâã€
ãã«âïŒâã€ãããã³ãžã«ã®â70âã®æº¶æ¶²ã66.5
mlã®ïœâããã«ãªããŠã ã®1.5M溶液ã§åŠçããã
â70âã«æŒããŠïŒåéã®åŸã100mlã®ããã©ãã
ããã©ã³äžã®8.0ïœã®äºéãš25.4ïœã®ãšãŠçŽ ãã
ã€ãããããšãŠåäºéã®æº¶æ¶²ãå ãããããçã
ã溶液ã¯â70âã«æŒããŠ20åéä¿ããããã®åŸ
5.6ïœïŒ0.1MïŒ6.65mlïŒã®ïŒâãããããŒã«ãâ
70âã§æ»ŽäžããŠå ããããã溶液ãâ70âã§30å
éä¿æããã次ã«7.8ïœïŒ0.1MïŒ70mlïŒã®å¡©åã¢
ã»ãã«ãå ããããã溶液ã宀枩ãŸã§æž©ãŸããã
ã«ãããšãŒãã«ã§åžéãéçé žãããªãŠã 氎溶液
ã§è¯ãæŽãã次ã«å¡©åãããªãŠã 氎溶液ã§æŽãã
ç¡«é žãã°ãã·ãŠã äžã§ä¹Ÿç¥ããŠèžçºããŠæ²¹ãæ®
ããããã200mlã®ã€ãœãããã«ã¢ã«ã³ãŒã«äžã§
åãããã10ïœïŒ0.093MïŒã®ããšãã«ããã©ãž
ã³ã§åŠçãããæ··åç©ãéæµãããªãã20åéå
ç±ããŠæ¬¡ã«æº¶åªãèžçºãããæ®æž£ã¯ã¯ãããã«ã
äžã«æº¶è§£ããã¯ãããã«ã ã§å å¡«ãããäºé žåã·
ãªã³ã³ã®ã«ã©ã ã«ããããããã¯ãããã«ã ã§æ¬¡
ã«ïŒïŒ ã¡ã¿ããŒã«ïŒã¯ãããã«ã ã§æº¶åºããŠïŒâ
ããªã¡ãã«ã·ãªã«ã¢ã»ãã¬ã³âïŒâã¢ããããâ
ïŒâãšã³âïŒâãªãŒã«ã®ã¢ã»ãã¢ãããåŸããã
ã30mlã®ãšã¿ããŒã«äžã«æº¶è§£ããŠ30mlã®æ°Žäžã®
2.5ïœã®æ°Žé žåã«ãªãŠã ã§å®€æž©ã«æŒããŠåŠçãã
ãããåŸã«ã¡ã¿ããŒã«ãæ¿Ÿå¥ãããæ°Žæ§æ®æž£ã¯å¡©
åãããªãŠã ã§é£œåããå¡©åã¡ãã¬ã³ã§è¯ãæœåº
ããããææ©å±€ã¯ç¡«é žãã°ãã·ãŠã äžã§ä¹Ÿç¥ãã
æ¿çž®ãããŠæ®æž£ãæ®ãããããã¯ãããã«ã ïŒç³
æ²¹ãšãŒãã«ã§åçµæ¶ã«ãããŠïŒâã¢ãããããµâ
ïŒâãšã³âïŒâã€ã³âïŒâãªãŒã«ïŒèç¹94âïŒã®
ã¢ã»ãã¢ãããåŸãããã®994mgïŒ6.5mMïŒã15
mlã®ããã©ããããã©ã³äžã«åããããŠæ°Žé žåã
ããªãŠã ã®50ïŒ æžæ¿æ¶²ïŒ0.5mMïŒ24mgã«å ããã
çŽ25âã«æŒããŠïŒååŸã溶液ã泚å°åšãã滎äžã
ãŠäºãâ23âã«å·ããããïŒãã©ã€ã¢ã€ã¹ïŒåå¡©
åççŽ ïŒ30mlã®ããã©ããããã©ã³äžã®935mg
ïŒ6.5mMïŒã®ããªã¯ããã¢ã»ããããªã«ã®æº¶æ¶²ã«
å ãããçãã溶液ã¯1.5æéâ23âã§æ¹æãã
ãŠã次ãã§çŽ25âã§èžçºãããŠæ²¹ãæ®ããããã
30mlã®ãã·ã¬ã³äžã«æº¶è§£ããŠéæµäžã«ïŒæéå ç±
ã次ã«çŽ25âã§äžå€æŸçœ®ãããçããæ²æŸ±ã¯éã
ãããã¯ãããã«ã ã§åçµæ¶ã6N HCl 40mlãš
ã¡ã¿ããŒã«100mlãšã«äžç·ã«ãããã溶液ã¯éæµ
äžã«12æéå ç±ããã次ã«æ¿çž®ããããçããæ®
枣ã¯ã¯ãããã«ã ã§è¯ãæŽããæšçã§åŠçãæ¿Ÿé
ããŠèžçºããŠæ®æž£ãæ®ããããããšã¿ããŒã«ã§å
çµæ¶ããŠïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãž
ã¢ãã³ãžãããã¯ãã©ã€ããèç¹175âïŒå解ïŒ
ãåŸãã å®æœäŸ ïŒ ïŒïŒïŒâãããâïŒâãšã³âïŒâã€ã³ãžã¢ãã³ 500mlã®ã¢ã³ã¢ãã¢äžã®2.3ïœã®ïŒ0.1MïŒãã
ãªãŠã ããé ããããããªãŠã ã¢ã»ããªãã®æº¶æ¶²
ã«ã35ïœïŒ35mMïŒã®ïŒâããããã·ãã³ãâïŒ
âãšããŒã«ãå ãããããäžæéåŸã«å¡©åã¢ã³ã¢
ããŠã ãå ããããã¢ã³ã¢ãã¢ã¯èžçºããããã«
ããããæ®æž£ã¯ãšãŒãã«äžã«ãšããããããæ¿Ÿé
ãããŠæ¿çž®ãããæ®æž£ãæ®ããããã200mlã®ã
ãã©ããããã©ã³äžã«ãšããããŠ48æéã25âã§
18.3ïœã®ïŒ70mMïŒããªããšãã«ãã¹ãã€ã³ã
12.1ïœïŒ70mMïŒã®ãžãšãã«ã¢ãŸãžã«ã«ããã·ã¬
ãŒãåã³10.2ïŒ70mMïŒã®ãã¿ã«ã€ãããšå ±ã«æ¹
æãããçããæ²æŸ±ãæ¿Ÿå»ããã¡ã¿ããŒã«ã§åçµ
æ¶ãã次ã«30mlã®ãšã¿ããŒã«äžã«æº¶è§£ããããšã¿
ããŒã«æº¶æ¶²ã¯ããã©ãžã³æ°Žåç©ïŒ1.74ïœïŒã§éæµ
äžã«äžå€åŠçãããã®åŸæº¶åªãèžçºããæ®æž£ãïŒ
ïŒ æ°Žé žåã«ãªã§å¡©åºã«ãŸã§åŠçãããžã¯ããã¡ã¿
ã³ã§æœåºããèžçºããŠèžçããŠïŒïŒïŒâãããâ
ïŒâãšã³âïŒâã€ã³ãžã¢ãã³ãåŸãã å®æœäŸïŒã®æé ã«æŒããŠïŒâãããããŒã«ãé©
åœéã®ïŒâããããŒã«ã«ããããšãã«ãïŒïŒïŒâ
ãããâïŒâãšã³âïŒâã€ã³ãžã¢ãã³äºå¡©é žå¡©ã
åŸãããã ODCã®äžå¯éçé»å®³ JACS100ã2551ã2553é ïŒ1978ïŒã«èšèŒãã
ãæ¹æ³ã§ãã©ã³ã¹ïŒïŒïŒâããã¹âïŒâãšã³âïŒ
âã€ã³ãžã¢ãã³ã®ã©ããèèãªã«ããã³ãã«ã«ã
ãã·ã©ãŒãŒäžæŽ»æ§åé床å®æ°ïŒKinactïŒã2.3Ã
10-3ã§ãã€ãããã®ããã«æ¬çºæã®ååç©ã¯
ODCäœçšãæããåŸã€ãŠæè «çãåã³å¢èïŒä¿
é²ïŒè¬æçµçšéã«å¯Ÿããæçšæ§ãæ¯æãããã
ãã¬ã³èªå°äœã§ããããšãæããã§ããã æ¬çºæååç©ã®è£œè¬åŠçã«åãå ¥ããããå¡©ã®
äŸãæããã°å¡©é žãèåæ°ŽçŽ é žãç¡«é žåã³çé žç
ã®ç¡æ©é žããŸãã¡ã¿ã³ã¹ã«ãã³é žããµãªãã«é žã
ãã¬ã€ã³é žãããã³é žãé ç³é žãã¯ãšã³é žãã¢ã¹
ã³ã«ãã³é žçã®ææ©é žã§åœ¢æãããç¡æ¯æ§é žä»å
å¡©ãåã³ã¢ã«ã«ãªéå±ãäŸãã°ãããªãŠã ãã«ãª
ãŠã ããªããŠã ãã¢ã«ã«ãªåé¡éå±ãäŸãã°ã«ã«
ã·ãŠã åã³ãã°ãã·ãŠã ã第æ軜éå±äŸãã°
ã¢ã«ãããŠã ã第äžçŽã第äºçŽåã¯ç¬¬äžçŽçã®æ
æ©ã¢ãã³é¡äŸãã°ã·ã¯ãããã·ã«ã¢ãã³ããšãã«
ã¢ãã³ãããªãžã³ãã¡ãã«ã¢ãããšã¿ããŒã«ããš
ã¿ããŒã«ã¢ãã³åã³ããã©ãžã³ã®å¡©åºçã®ç¡æ©å
ã¯ææ©å¡©åºã§åœ¢æãããç¡æ¯æ§å¡©ãå«ãŸãããå¡©
ã¯æ £çšã®æ段ã«ãã€ãŠåœ¢æãããã ãã¡ãã¬ã³åã¯ãšããªãã³ã§ããååç©é¡ã
奜ãŸããã¯ããã¡ãã¬ã³ã§ããååç©ã¯ãã奜
ãŸããã æ¬çºæååç©ã®äŸãæããã°ä»¥äžã®éãã§ã
ããïŒæ³šïŒä»¥äžããã¹ã¯ïŒhexïŒã®èš³ã§ãããã
ã»ãšã¯ããªãã€ãã ïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ã ïŒïŒïŒâãããâïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ã ïŒïŒïŒâãããâïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ã æ¬çºæååç©ã®å©çšåé (ã€) äžè¬åŒïŒã®ååç©é¡ã¯ããªã¢ãã³åœ¢æã«ä¿ã
ã«ã«ããã·ã«åºåè§£é µçŽ ã®äžå¯éçé»å®³å€ã§ã
ãè¬çåŠçè©Šè¬ãšããŠãã®ååç©ã¯æçšã§ã
ããããªã¢ãã³ãšãããããã¬ã¹ã·ã³ãã¹ãã«
ããžã³åã³ã¹ãã«ãã³ã¯æ€ç©åã³åç©çµç¹ã«å
åšããŸããã埮çç©äžã«ãååšãããããªã¢ã
ã³é¡ã®æ£ç¢ºãªççåŠç圹å²ã¯æ確ã«ã¯èšè¿°ã¯ãª
ãããããªã¢ãã³ã现èåè£åã³çé·ã«ä¿ãã
ãã€ããšã瀺åãã蚌æ ãããïŒãšã€ã ãžâ
ãŠã€ãªã¢ã ãºâã¢ã·ãŠãã³çïŒH.G.
WilliamsâAshman et alïŒãThe ltalian J.
Biochem.25ïŒïŒâ32ïŒ1976ïŒããšã€ã©ã€ã ã¢
ã³ã ãžãšãŒ ãžãšãŒã³ïŒA.Raina and J.
JanneïŒãMed.Biol.53ïŒ121â147ïŒ1975ïŒåã³
ãã€ãŒ ãšã€ã ã©ãã»ã«ïŒD.H.RussellïŒã
Life Science 13ïŒ1635â1647ïŒ1973ïŒãããªã¢
ãã³ã¯äŸãã°ã€ãŒ ã³ãªïŒE.coliïŒããšã³ãã
ãã¯ã¿ãŒïŒEnterobacterïŒãã¯ã¬ãã·ãšã©
ïŒKlebsiellaïŒãã¹ã¿ãã€ãã³ãã«ã¹ãªãŒã¬ãŠã¹
ïŒStaphylococcus aureusïŒãã·ãŒ ã«ãããªã¹
ïŒC.cadaverisïŒããµã«ã¢ãã©ã¯ã¿ã€ããªãµ
ïŒSalmonella typhosaïŒåã³ããšã¢ãã€ã©ã¹ã
ã©ã€ã³ãã«ãšã³ã¶ïŒHaemophilus
parainfluenzaïŒãªã©ããçš®ã®åŸ®çç©ã«å¯Ÿãã
å¿ é çé·å åã§ãããåã¯çé·éçšã«ä¿ããæ
ãããããªã¢ãã³ã¯çŽ°èå¢æ®ãèµ·ããåºæ¿ã«ç¶
ããŠåæåã³èç©ã®å¢å ãããã®ã§æ£åžžãªçé·
åã³æ°çç©ã®æ¥çé·ã®äž¡æ¹å ±ã«é¢ä¿ãããããŸ
ããããªã¢ãã³æ°Žæºã¯èçµç¹ãçœè¡ç 现èåã³
ä»ã®æ¥æé·çµç¹ã«æŒããŠé«ãããšãç¥ãããŠã
ãããªã«ããã³ãâã¢ããã·ã«ã¡ããªãã³ã
ã¢ã«ã®ãã³åã³ãªãžã³ã®ã«ã«ããã·ã«åºåè§£é µ
çŽ ã®æŽ»æ§ãšããªã¢ãã³åœ¢æãšã®éã«çžé¢é¢ä¿ã
ããããšãç¥ãããŠããã ããã¬ã·ã³ãã¹ãã«ããžã³åã³ã¹ãã«ãã³ã®
çåæã¯çžäºã«é¢ä¿ããŠãããããã¬ã·ã³ã¯ãª
ã«ããã³ã«ã«ããã·ã«åºåè§£é µçŽ ã«ãã觊åªã
ãããªã«ããã³ã®è±ã«ã«ããã·ã«åïŒè±çé žïŒ
çæç©ã§ãããããã¬ã·ã³çæã¯ãŸãã¢ã«ã®ã
ã³ãè±çé žãããŠã¢ã°ããã³ãçãããããå
æ°Žå解ãããŠããã¬ã·ã³ãšå°¿çŽ ãçæããããš
ã«ãã€ãŠãçãåŸããã¢ã«ã®ãã³ããŸãé µçŽ ã¢
ã«ã®ããŒãŒã®äœçšã«ãã€ãŠãªã«ããã³åœ¢æã«ä¿
ã€ãŠããããšã¹âã¢ããã·ã«ã¡ããªãã³ã·ã³ã»
ã¿ãŒãŒã«ããã¡ããªãã³ã®æŽ»æ§åãâã¢ãã
ã·ã«ã¡ããªãã³ã圢æããããã¯è±çé žããã
ãããã®ã¡ã«æŽ»æ§åãããã¡ããªãã³ã®ããã
ã«ã¢ãã³éšåãããã¬ã·ã³ã«ç§»ãããããšãåº
æ¥ãã¹ãã«ããžã³ã圢æããã¹ãã«ããžã³ãã¹
ãã«ãã³ã圢æãããåŸã€ãŠããã¬ã·ã³ãã¹ã
ã«ããžã³åã³ã¹ãã«ãã³ã®åé§äœãšããŠåãã
æŽã«ãããã¬ã·ã³ã®åæå¢å ã¯çµç¹ãæ¹æ°ãã
ãçé·éçšãåããæåã®åŸŽåã§ããããšã瀺
ãããŠãããšããç¹ã«æŒããŠããããããªã¢ã
ã³çåæçµè·¯ã®é¡èãªå¶åŸ¡å¹æãæããããšã
瀺ããŠããããªãžã³ã®è±çé žçæç©ã§ããã«ã
ããªã³ã¯ïŒ³âã¢ããã·ã«âã¡ããªãã³ã«ã«ãã
ã·ã«åºåè§£é µçŽ ã®æŽ»æ§ãåºæ¿ããããšã瀺ãã
ãŠããããŸãå€ãã®åŸ®çç©ãäŸãã°ãšã€ã ã
ã©ã€ã³ãã«ãšã³ã¶ïŒH.parainfluenzaïŒã®çé·
éçšã«å¿ é ã§ããããšãç¥ãããŠããã (ã) åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšããªãã³ã§
ããååç©ã¯ããçš®ã®æ¥æé·éçšãæå¶ããã®
ã«ãæçšã§ãããäŸãã°è©²ååç©ã¯ç²Ÿå圢æå
ã³è圢æã®é»å®³ã«æçšã§ãããåŸã€ãŠéã®å粟
é»æ¢å€åã³å èè¬ãšããŠã®çšéãèŠåºããŠã
ãããã®ååç©ã¯ãŸãæ°çç©çé·äŸãã°å å®æ§
è «çãçœè¡ç ããªã³ãè «ã®æå¶ã«æçšã§ããã
äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšãã¬ã³ã§
ããååç©ãæäžããã«æŒããŠã¯ãåæã«æ¢ç¥
ã®æé ã«ãã€ãŠãã©ã³ã¹ïŒÂ±ïŒâïŒâããšãã«
ã·ã¯ããããããã³ïŒtransïŒÂ±ïŒâïŒâphenyl
âcycloproponamineïŒåã¯ïŒ®âãã³ãžã«â
âã¡ãã«âïŒâããããã«ã¢ãã³çã®ã¢ãã¢ã
ã³ãªãã·ããŒãŒé»å®³å€ãæäžããã®ãæãŸãã
ãããããªããäžè¬åŒïŒååç©ã®ãªã«ããã³å
ã¯ïŒ³âã¢ããã·ã«ã¡ããªãã³ã«ã«ããã·ã«åºå
è§£é µçŽ ã®äžå¯éçé»å®³å€ãšããŠã®æçšæ§ã¯æ¬¡ã®
æ§ã«ããŠæž¬å®ã§ãããé©åœãªååç©ã®æ°Žæº¶æ¶²ã
çµå£çåã¯éçµå£çã«éã©ããåã¯ããŠã¹ã«äž
ãããããååç©æäžåŸïŒä¹è³48æéåŸã«åç©
ã殺ãåç«è ºã®è ¹åŽèãé€å»ããå質åãããª
ã«ããã³åã³ïŒ³âã¢ããã·ã«ã¡ããªãã³ã«ã«ã
ãã·ã«åºåè§£é µçŽ æŽ»æ§ãã€ãŒ ãšãŒ ããã°
ïŒE.A.PeggïŒåã³ãšã€ã ãžãŒ ãŠã€ãªã¢ã ã¹
âã¢ãã·ãŠãã³ïŒH.G.WilliamsâAshmanïŒã
Biochem.J.108ïŒ533â539ïŒ1968ïŒåã³ãžãšãŒ
ãžãšãŒã³ïŒJ.JanneïŒåã³ãšã€ã ãžãŒ ãŠ
ã€ãªã¢ã ã¹âã¢ãã·ãŠãã³ãBiochem.and
Biophys.Res.Comm.42 222â228ïŒ1971ïŒã«æŠ
ç¥çã«èšèŒãããæ§ã«æž¬å®ãããã (ã) äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšãã¬ã³
ã§ããååç©ã¯æ¬¡ã®æ§é ïŒåŒäžïŒã¯ïŒåã¯ïŒïŒãæããååç©ã®ä»£è¬
åé§äœã§ãããåŒïŒã®ååç©ã¯Î³âã¢ããé ªé ž
ãã©ã³ã¹ã¢ãããŒãŒã®äžå¯éçé»å®³å€ãšããŠç¥
ãããæäžã«ãã€ãŠÎ³âã¢ããé ªé žïŒGABAïŒ
ã®é«ãè³å æ°Žæºãçããã (ã) äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšãã¬ã³
ã§ããååç©ã¯åŒïŒã®ååç©ã«ä»£è¬çã«å€æã§
ããããšã¯ãçŸåšæãŠããã掻æ§ãç«èšŒããã®
ã«çšããããŠããã·ã ã©ãŒïŒSimlerïŒçã
Biochem.Pharmacol.22ïŒ1701ïŒ1973ïŒã«ãã
èšèŒãããäžè¬æ¹æ³ã«ãã€ãŠæž¬å®ãããDBA
系統ã®ããŠã¹ã®èŽåæ§ã®æ¥çºäœã«å¯Ÿãããã®å
åç©ã®ä¿è·äœçšã«ãã€ãŠäŸç€ºãããããšãåºæ¥
ãã ããã (ã) äžè¬åŒïŒã®ååç©ã¯æ¬¡ã®äžè¬åŒïŒã®æ°èŠãªã»
ãã¢ãã¹ããªã³èªå°äœã®è£œé ã®ååŠäžéäœç©è³ª
ãšããŠæçšã§ãããåŒïŒã®ã»ãã¢ãã¹ããªã³å
åç©ã¯æçç©è³ªãšããŠæçšã§ããã äžã®äžè¬åŒïŒã«æŒããŠïŒ¡ã¯äžè¬åŒïŒã§ã®å®çŸ©
ãšåãæå³ãæã¡ãïŒã¯æ°ŽçŽ åã¯è² é»è·ããŸã
ã¯æ°ŽçŽ åã¯ã¢ã»ããã·ã§ããã äžè¬åŒïŒã®ååç©åã³ãããã®è£œè¬åŠçã«å
ãå ¥ããããå¡©åã³åã ã®å åŠç°æ§äœã¯æçç©
質ãšããŠæçšãªæ°èŠãªååç©ã§ãã€ãŠå€ãã®è¯
ãç¥ãããã»ãã¢ãã¹ããªã³èªå°äœäŸãã°ã»ã
ã¢ã¬ãã·ã³ãã»ãã¢ããã³ãåã¯ã»ãã¢ãã°ãª
ã·ã³ãšåæ§ã®æ¹æ³ã§æäžãããããšãåºæ¥ãã
äžè¬åŒïŒã®ååç©åã³ãããã®è£œè¬åŠçã«åã
ãããããå¡©åã³ç°æ§äœé¡ã¯åç¬ã§åã¯è£œè¬åŠ
çåŠæ¹å€ãšããŠçµå£çåã¯éçµå£çåã³å±æç
ã«æž©è¡åç©å³ã¡é³¥åã³åºä¹³é¡ãäŸãã°ç«ãç¬ã
çãçŸã銬åã³äººéã«æäžãããããšãåºæ¥
ããçµå£æäžãšããŠã¯æ¬ååç©ã¯é å€ãã«ãã»
ã«å€ãåã¯äžžè¬ã®åœ¢ã§åã¯ãšã«ããžãŒã«åã¯æž
æ¿å€ã®åœ¢ã§æäžãããããéçµå£æäžã«ã¯ãæ¬
ååç©ã¯ä»ã®æº¶è³ªäŸãã°æº¶æ¶²ãç匵ã«ãããã
ã®å åãªå¡©æ°Žåã¯ã°ã«ã³ãŒã¹ãå«ã¿ããæ» èæ°Ž
溶液ã®åœ¢ã§äœ¿çšãããã®ãæãè¯ãã§ãããã
å±ææäžã«ã¯ãäžè¬åŒïŒã®ååç©åã³ãããã®
å¡©åã³ç°æ§äœé¡ã¯ã¯ãªãŒã åã¯è»èäžã«æ··å ¥ã
ããã äžè¬åŒïŒã®ååç©åã³ãããã®è£œè¬åŠçã«å
ãå ¥ããããå¡©é Œåã³åã ã®å åŠç°æ§äœé¡ã察
æãã掻æ§ãæãã埮çç©ã®äŸãæããã°ãã¹
ã¿ãã€ãã³ãã«ã¹ ãªãŒã¬ãŠã¹
ïŒStaphylococcus aureusïŒããµã«ã¢ãã© ã·ãš
ããã ãšã¬ãªïŒSalmonella schotmuehleriïŒã
ã¯ã¬ãã·ãšã© ããŠãŒã¢ãã¢ïŒKlebsiella
pneumoniaeïŒããã€ããã³ãã«ã¹ ããŠãŒã¢
ãã¢ãšïŒDiplococcus pneumoniaeïŒåã³ã¹ã
ã¬ããã³ãã«ã¹ ããªã²ãã¹ïŒStreptococcus
pyogenesïŒã§ããã äžè¬åŒïŒã®ååç©ã®è£œè¬åŠçã«åãå ¥ããã
ãç¡æ¯æ§ã®ç¡æ©é žä»å å¡©ãäŸç€ºããã°ãé±é žä»
å å¡©äŸãã°å¡©é žãèåæ°ŽçŽ é žå¡©ãç¡«é žå¡©ãã¹ã«
ãã¢ãã³é žå¡©ãçé žå¡©åã³ææ©é žä»å å¡©äŸãã°
ãã¬ã€ã³é žå¡©ãé ¢é žå¡©ãã¯ãšã³é žå¡©ãä¿®é žå¡©ã
ãã¯ãé žå¡©ãå®èéŠé žå¡©ãé ç³é žå¡©ããããŒã«
é žå¡©ãææªé žå¡©åã³ã¢ã¹ã³ã«ãã³é žå¡©ã§ããã
å¡©é¡ã¯æ £çšã®æ段ã«ãã€ãŠã€ããããšãåºæ¥
ãã äžè¬åŒïŒã®ååç©ã®äŸãæããã°ïŒæ¬æ现æž
äžãã³ãã¯ïŒpentïŒãããã¯ïŒbutïŒããªã¯ãã¯
ïŒoctïŒã®èš³ã§ãããïŒ ïŒâïŒâïŒâïŒïŒâã¢ã»ãã¬ã³âïŒâã¢ã
ãããâïŒâãšãã«ã¢ããã¡ãã«ïŒããšãã«ïŒœ
ã¢ã»ãã«ïŒœã¢ããâïŒâã¢ã»ãããã·ã¡ãã«
âïŒâãªããœâïŒâãã¢âïŒâã¢ã¶ãã·ã¯ã
ïŒïŒïŒïŒïŒïŒœãªã¯ãâïŒâãšã³âïŒâã«ã«ã
ã³é žã§ããã æäžæ¹æ³ïŒœ è¬çåŠçã«æçšãªè¬å€ãšããŠäžè¬åŒïŒã®ååç©
ã¯ææã®å¹æãéæããããã«æ²»çãããæ£è ã«
çš®ã ã®æ¹æ³ã§æäžãããããè¬çåŠçã«æçšãªæ¬
çºæååç©ã¯åç¬ã§åã¯ä»ãšã®çµã¿åããã§äœ¿çš
ããããããŸããæ¬çºæã®è¬çåŠçã«æçšãªåå
ç©ã¯ã補è¬åŠçãªåŠæ¹å€ã®åœ¢ã§æäžãããŠãè¯
ããååç©ã¯çµå£çã«ãéçµå£çã«ãäŸãã°éè
å ãè ¹è å åã¯ç®äžã«ãããåã¯å±æçã«æäžã
ããããæäžãããååç©ã®éã¯åºãç¯å²ã«ãã€
ããŠå€ããã§ãããããä»»æã®æå¹éã§ããã
ããæ²»çãããæ£è ãæ²»çãã¹ãçç¶ãåã³æäž
æ¹æ³ã«äŸåããŠãååç©ã®æå¹éã¯åäœé©éåœã
æ£è ã®äœéããã°ã©ã åœãçŽ0.1mgä¹è³500mgã§å€
åãã奜ãŸããã¯åäœé©éåœãæ£è ã®äœéããã°
ã©ã åœãçŽ10mgä¹è³çŽ100mgã奜ãŸããã§ãããã
äŸãã°å žåçãªåäœæäžåœ¢åŒã¯åŒïŒã®ååç©10ä¹
è³300mgãå«ãé å€ã§ãã€ãŠææã®å¹æãéæã
ãããã«ã¯æ²»çãããæ£è ã«ïŒæ¥ïŒä¹è³ïŒåæäž
ãããããšãåºæ¥ããããã«äœ¿çšãããæ£è ã®çš
èªã¯åºä¹³é¡äŸãã°ç«ãç¬ãã©ãããããŠã¹ãã¢ã«
ã¢ããã銬ãçãçŸåã³äººéçã®æž©è¡åç©ãæå³
ããæ§ã«äœ¿çšãããã åºäœã®é©éåäœåœ¢åŒã¯æ £çšã®ãã®ã§ããããšã
åºæ¥ããåºäœåœ¢åŒã¯æ¬çºææ°èŠååç©ãšæ äœäŸã
ã°æ»å€åã³ä¹³ç³ãã·ãšç³åã³ã³ãŒã³ã¹ã¿ãŒãçã®
äžæŽ»æ§ã®å å¡«å€ãå«ãã æ®éã®ãŒã©ãã³åã®ãã®
ã§ããããã»ãã»ã«å€ã§ããããšãåºæ¥ããå¥ã®
å ·äœäŸã§ã¯æ°èŠååç©ã¯ä¹³ç³ãã·ãšç³åã¯ã³ãŒã³
ã¹ã¿ãŒãçã®éåžžã®é å€ããŒã¹ãšã¢ã«ã·ã¢ãã³ãŒ
ã³ã¹ã¿ãŒãåã¯ãŒã©ãã³çã®çµåå€ãã³ãŒã³ã¹ã¿
ãŒãããžã€ã¬ã€ã¢æŸ±ç²ãåã¯ã¢ã«ã®ã³é žçã®åŽ©å£
å€åã³ã¹ãã¢ãªã³é žåã¯ã¹ãã¢ãªã³é žãã°ãã·ãŠ
ã çã®æ»å€ãšã®çµã¿åããã§é å€åãããã éçµå£æäžã«ã¯ãæ¬ååç©ã¯ççåŠçã«èªãã
ãåžéå€äžã®æ¬ååç©ã®æº¶æ¶²åã¯æžæ¿æ¶²ã®ãè¡šé¢
掻æ§å€åã³ä»ã®è£œè¬äžèªãããäœè¬ãæ·»å ããå
ã¯æ·»å ããªãæ°Žåã¯æ²¹çã®æ» è液äœã§ãããã補
è¬åŠçæ äœãå«ãã 泚å°å¯èœãªé©é圢åŒãšããŠæ
äžããããããããã®åŠæ¹å€äžã«çšãããããæ²¹
ãäŸç€ºããã°ãç³æ²¹ãåç©ãæ€ç©åã¯åæèµ·æºã®
ãã®äŸãã°ããŒãããæ²¹ã倧è±æ²¹åã³é±æ²¹ã®ãã®
ã§ãããäžè¬ã«ãæ°Žãå¡©æ°Žãæ°Žæ§ããã¹ãããŒã¹
åã³é¢é£ããç ç³æº¶æ¶²ããšã¿ããŒã«åã³ãããã¬
ã³ã°ãªã³ãŒã«åã¯ããªãšãã¬ã³ã°ãªã³ãŒã«ãªã©ã®
ã°ãªã³ãŒã«é¡ã¯å¥œãŸãã液äœæ äœã§ããç¹ã«æ³šå°
å¯èœæº¶æ¶²ã«ã¯å¥œãŸããã æ¬ååç©ã¯æŽ»æ§æåã®æç¶æ§æŸåºãå¯èœã«ãã
æ§ãªæ¹æ³ã§åŠæ¹ãããã貯èµæ³šå°ïŒdepot
injectionïŒåã¯æ¿å ¥åŠæ¹å€ã®åœ¢åŒã§æäžããã
ããšãåºæ¥ãã掻æ§æåã¯ãã¬ããåã¯å°ããªç
ã«å§çž®ããç®äžã«åã¯çèå ã«è²¯èµæ³šå°åã¯ã€ã³
ãã©ã³ããšããŠæ¿å ¥ããããã€ã³ãã©ã³ãã¯çç©
å解å¯èœãªéåäœåã¯åæã·ãªã³ã³é¡äŸãã°ããŠ
ã³ãŒãã³ã°ç€Ÿã«ãã補é ãããã·ãªã³ã³ãŽã ã®ã·
ã©ã¹ãã€ãã¯ïŒSilasticïŒãªã©ã®äžæŽ»æ§ç©è³ªãçš
ããããšãåºæ¥ãã 補æ³ïŒœ äžè¬åŒïŒã«æŒããŠïŒ¡ãã¡ãã¬ã³åã¯ãšããªãã³
ã§ããååç©ã¯ãä»»æã«ïŒäŸ¡ã®éå±ã«ããªã³äŸã
ã°ãšãŠåäºéãåã¯èåãã°ãã·ãŠã ã®ååšã®äž
ã«ãïŒåœéã®é©åœã«ä¿è·ããããããã«ã®ã«ã¢ã
ã³ã匷塩åºã§åŠçããŠãä¿è·ããããããã«ã®ã«
ã¢ãã³ãã«ã«ãããªã³äžéäœãçæãããããïŒ
âãããããŒã«åã¯ããããŒã«ã§ã¢ã«ãã«åããŠ
ããã²ã³åã¢ã«ã«ãã€ã«äŸãã°å¡©åã¢ã»ãã«åã¯
å¡©åããããªãã«ãåã¯å¡©åãã³ãŸã€ã«ã®æ§ãªã
ãã²ã³åã¢ããŒã€ã«ãåã¯äœçŽã¢ã«ãã«ããããŒ
ã¡ãŒãçã®é žããã²ã³åç©åã¯ç¬¬ïŒçŽãããã·ã«
ã«ããã«ã¢ãžãã§ã¢ã·ã«åããç¶ãã§ïŒâã¢ãã
âïŒâããªã¡ãã«ã·ãªã«ã¢ã»ãã¬ã³ããâïŒâãš
ã³âïŒâãªãŒã«ã®ã¢ããåã¯ã«ã«ãã¡ãŒãã«å æ°Ž
å解ãããããéçé žãããªãŠã åã¯éçé žã«ãª
ãŠã ãçé žãããªãŠã åã¯çé žã«ãªãŠã ãæ°Žé žå
ãããªãŠã åã¯æ°Žé žåã«ãªãŠã çã®å¡©åºã§åŠçã
ãŠïŒâã¢ããããã¹âïŒâãšã³âïŒâã€ã³âïŒâ
ãªãŒã«ã®ã«ã«ããã·ã¢ãããåŸãããã溶åªäŸã
ã°ãžãšãã«ãšãŒãã«ãããã©ããããã©ã³ããžãª
ããµã³ããžã¡ããã·ãšã¿ã³ãªã©ã®ãšãŒãã«é¡ãã
ã³ãŒã³åã¯ãã«ãšã³ãªã©ã®çåæ°ŽçŽ äžã§æ°ŽçŽ åã
ããªãŠã ãã«ãªãŠã 第ïŒãããã·ãããªããŠã ã¢
ã«ãã«ã¢ããäŸãã°ãªããŠã ãžã€ãœãããã«åã¯
ã¢ã«ãã«ãªããŠã ãªã©ã®è§Šåªéã®å¡©åºã®ååšäž
ã«ãçŽâ30ããïŒâã«æŒããŠçŽ30åãïŒæéããª
ã¯ããã¢ã»ããããªã«ã§åŠçããããšã«ãããã
ãªã¯ããã¡ãã«ã€ãããŒããšã¹ãã«ãåŸãããã
çŽ110ãã140âã«æŒããŠé極æ§æº¶åªäŸãã°ãã·ã¬
ã³ããã«ãšã³ãããããã³ãŒã³åã¯ã¯ãããã³ãŒ
ã³äžã§çŽïŒã10æéå ç±ããŠããªã¯ããã¡ãã«ã¢
ã»ãã¢ãããåŸããããé žæ°Žæº¶æ¶²äŸãã°å¡©é žåã¯
å¡©åºæ°Žæº¶æ¶²äŸãã°æ°Žé žåãããªãŠã åã¯æ°Žé žåã«
ãªãŠã ãçšããŠå æ°Žå解ããããšã«ãã€ãŠè£œé ã
ããã äžè¿°ã®ã¢ã«ãã«ååã¯ã¢ã·ã«ååå¿ã¯äžæ§æº¶åª
äŸãã°ãã³ãŒã³ããã«ãšã³ããšãŒãã«ãããã©ã
ãããã©ã³ããžã¡ãã«ã¹ã«ããã·ãåã¯ãããµã¡
ãã«ãã¹ãã«ããªã¢ããäžã§è¡ããããåå¿æž©åºŠ
ã¯â125ãä¹è³25âã§çŽ30åã24æéã®éã§å€åã
ããã ïŒâã¢ããâïŒâããªã¡ãã«ã·ãªã«ã¢ã»ãã¬ã³
ããâïŒâãšã³âïŒâãªãŒã«ã®ã¢ãããåŸããã
ã®å æ°Žå解ã¯ããã©ãžã³ãããšãã«ããã©ãžã³å
ã¯ããããã·ã«ã¢ãã³ã§åŠçããããšã«ããåã¯
é±é žäŸãã°å¡©é žã§åŠçããŠç¶ããŠããªã¡ãã«ã¢ã
ã³åã¯ããªãžã³çã®ææ©å¡©åºã§ã¡ã¿ããŒã«åã¯ãš
ã¿ããŒã«çã®äœçŽã¢ã«ã³ãŒã«æ§æº¶åªäžã«æŒããŠçŽ
80ã110âã§30åãïŒæéåŠçããããšã«ããé
æãããã äžã®åå¿ã§çšããããé©åœã«ä¿è·ãããããã
ã®ã«ã¢ãã³ã¯æ¬¡ã®äžè¬åŒïŒã§è¡šããããã åŒäžR8ã¯ççŽ ååïŒãïŒåãæããçŽéåã¯
åå²éã¢ã«ãã«ãäŸãã°ã¡ãã«ããšãã«ãïœâã
ããã«åã³ç¬¬äžâããã«åã¯ããªãšãã«ã¡ãã«ã§
ãããåŒïŒã®ååç©ã¯ãããã®ã«ã¢ãã³ã®ã¢ã»ã
ã¬ã³åºåã³çªçŽ å®èœåºäžã«ä¿è·åºãä»å ããŠè£œé
ãããããããã®ã«ã¢ãã³ã®çªçŽ å®èœåºã®ä¿è·ã¯
æ¢ç¥ã®æ¹æ³ã«ãããã³ãºã¢ã«ããããïŒïŒïŒâãž
ã¡ãã«ãããããŒã«åã³ïŒïŒïŒâãžãšãã«ãã¿ã
ãŒã«ããéžã°ããéãšããŒã«ååã«ã«ããã«å«æ
ååç©ã§ã·ããå¡©åºã圢æããŠè¡ãªããããã¢ã»
ãã¬ã³å®èœåºã®ä¿è·ã¯äžè¿°ã®ã·ããå¡©åºãã¢ã«ã
ã«éšåãççŽ ååïŒãïŒåãæãçŽéåã¯åå²é
ã®ããªã¢ã«ãã«ã·ãªã«ã¯ãã©ã€ãäŸãã°ããªã¡ã
ã«ã·ãªã«ã¯ãã©ã€ãåã¯ããªãšãã«ã·ãªã«ã¯ãã©
ã€ããšåå¿ããæ¢ç¥ã®æ¹æ³ã«ãã察å¿ããããªã¢
ã«ãã«ã·ãªã«èªå°äœã圢æããããšã«ããéæã
ããã ã«ã«ãããªã³ã圢æããããã«äžã®åå¿ã§çšã
ãããé©åœãªåŒ·å¡©åºã¯ã¢ã«ãã«ãªããŠã äŸãã°ã
ãã«ãªããŠã ãåã¯ããšãã«ãªããŠã ããªããŠã
ãžã¢ã«ãã«ã¢ããäŸãã°ãªããŠã ãžã€ãœãããã«
ã¢ããããªããŠã ã¢ããã第ïŒçŽã«ãªãŠã ããã¬
ãŒãåã¯ãããªãŠã ã¢ããçã®ã¢ã»ãã¬ã³éšåã«
é£æ¥ããççŽ ååãããããã³ãæãåããã®ã§
ããã äžè¬åŒïŒã«æŒããŠãããšãã¬ã³ã§ããååç©
ã¯ïŒâããããã·ãã³ãâïŒâãšããŒã«ãåŒ
HCCMâ²ïŒåŒäžMâ²ã¯ãããªãŠã ããªããŠã åã¯
MgXâ²ã§ãããããã§Xâ²ã¯å¡©çŽ åã¯èçŽ ã§ããïŒ
ã®éå±ã¢ã»ããªãã§åã¯æ¶²äœã¢ã³ã¢ãã¢ããžã¡ã
ã«ã¹ã«ããã·ãããšãŒãã«é¡äŸãã°ããã©ããã
ãã©ã³ããžãªããµã³ããžãšãã«ãšãŒãã«åã¯ãžã¡
ããã·ãšã¿ã³ãªã©ã®æº¶åªäžã®ãªããŠã ã¢ã»ããª
ãïŒãšãã¬ã³ãžã¢ãã³ã®é¯äœã§çŽâ30ãã25âã«
æŒããŠçŽïŒåãïŒæéåŠçããŠãããâïŒâãšã³
âïŒâã€ã³âïŒïŒïŒâãžãªãŒã«ãåŸãããšã«ãã
補é ãããããããªãŠã åã¯ãªããŠã ã¢ã»ããªã
ãçšãããããšãã«ã¯æ¶²äœã¢ã³ã¢ãã¢ã奜ãŸãã
溶åªã§ããããªããŠã ã¢ã»ããªããçšãããããš
ãã¯ãšãŒãã«æº¶åªã奜ãŸããããšãŒãã«æº¶åªã¯å¥œ
ãŸããåå¿æž©åºŠçŽïŒã25âã§ããã²ã³åãã°ãã·
ãŠã ãçšãããããšãã«å¥œãŸããããªããŠã ã¢ã»
ããªãâãšãã¬ã³ãžã¢ãã³é¯äœãçšãããããšã
ã«ã¯ã枩床25âãæéçŽïŒã12æéãçšããŠå¥œãŸ
ãã溶åªããžã¡ãã«ã¹ã«ãããµã€ãã§ããã ãžãªãŒã«èªå°äœã¯ãã¿ã©ãããããªããšãã«ã
ã¹ãã€ã³åã³ãžãšãã«ãžã¢ãŸãžã«ã«ããã·ã¬ãŒã
ã§ããã©ããããã©ã³ããžãšãã«ãšãŒãã«åã¯ãž
ãªããµã³ãªã©ã®ãšãŒãã«äžã«æŒããŠçŽïŒã12æé
çŽ25ãã50âã§åŠçããã察å¿ãããžãã¿ã«ã¢ã
ãèªå°äœãäžããããã¯ã¡ã¿ããŒã«åã¯ãšã¿ããŒ
ã«ãªã©ã®äœçŽã¢ã«ã³ãŒã«æº¶åªäžã§ããã©ãžã³æ°Žå
ç©ã«ããçŽïŒãïŒæéçŽ25ãã50âã§åŠçããã
次ãã§é žäŸãã°6N HClã§100âãïŒã10æéåŠ
çãããã åèäŸ ïŒäžéäœãšããŠã®çšéïŒ ïŒâïŒâïŒâïŒïŒâã¢ã»ãã¬ã³âïŒâã¢ãã
ãã³ãâïŒâãšãã«ã¢ããã¡ãã«ïŒããšãã«ïŒœ
âã¢ã»ãã«ïŒœã¢ããâïŒâã¢ã»ãããã·ã¡ã
ã«âïŒâãªããœâïŒâããªâïŒâã¢ã¶ãã·ã¯ã
âïŒïŒïŒïŒïŒïŒœãªã¯ãâïŒâãšã³âïŒâã«ã«
ãã³é ž 50mlã®ãšã¿ããŒã«äžã®ïŒïœã®ïŒâã¢ã»ãããã·
ã¡ãã«âïŒâïŒâïŒâã¯ããã¡ãã«ïŒããšã
ã«ïŒœã¢ã»ãã«ïŒœã¢ããâïŒâãªããœâïŒâãã¢
âïŒâã¢ã¶ãã·ã¯ãïŒïŒïŒïŒïŒïŒœâãªã¯ãâïŒ
âãšã³âïŒâã«ã«ãã³é žåã³ã¢ã»ãã¬ã³å®èœåºã«
察ããŠæ«ç«¯ã®ã¢ããåºããã¿ã«ã€ãããšããŠä¿è·
ãããŠããïŒïœã®ïŒïŒïŒâãããâïŒâãšã³âïŒ
âã€ã³ãžã¢ããã®æ··åç©ã25âã§24æéæ¹æããŠ
ãã溶åªãé€å»ããŠæ®æž£ãæ®ãããããããã©ãž
ã³ã§åŠçããŠæº¶åºæ¶²ãšããŠãã³ãŒã³âã¢ã»ãã³ã
çšããŠã·ãªã«ã²ã«äžã§ã¯ãããã°ã©ãã«ããïŒâ
ïŒâïŒâïŒâã¢ã»ãã¬ã³âïŒâã¢ãããã³ã
âïŒâãšãã«ã¢ã»ãã«ïŒœã¢ããâïŒâã¢ã»ãã
ãã·ã¡ãã«âïŒâãªããœâïŒâãã¢âïŒâã¢ãµã
ã·ã¯ãâïŒïŒïŒïŒïŒïŒœãªã¯ãâïŒâãšã³âïŒâ
ã«ã«ãã³é žãåŸãã 以äžã«äžè¬åŒïŒã®ååç©ã®è£œè¬åŠçåŠæ¹å€ãäŸ
瀺ããã 硬質ãŒã©ãã³ã«ãã»ã«ã®çµæã¯ä»¥äžã®æ§ã«äŸç€º
ãããã (a) ïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³ 20mg (b) æ»ç³ ïŒmg (c) ä¹³ç³ 90mg åŠæ¹å€ã¯(a)ãš(b)ã®ä¹Ÿç¥ç²æ«ã现ã¡ãã·ãŠã®ç¯©ã«
éããããããååæ··åããããšã«ãã€ãŠé ãã
ããç²æ«ã¯æ¬¡ã«ç¡¬è³ªãŒã©ãã³ã«ãã»ã«ã«æ£å³å å¡«
éã«ãã»ã«åœã115mgã§ã€ããããã 泚å°çšæžæ¿æ¶²çšã®çµæãäŸç€ºãããã®ã¯ä»¥äžã®
çèå 泚å°çšã®ïŒmlã®ã¢ã³ãã«ã§ããã ééããŒã»ã³ã (a) ïŒïŒïŒâãããâïŒâãšã³â âïŒâã€ã³ãžã¢ãã³ 1.0 (b) ããªããã«ãããªãã³ 0.5 (c) ã¬ã·ãã³ 0.25 (d) 100ã«ãã泚å°çšæ°Ž (a)ãš(b)ã®ç©è³ªãæ··åããå質ã«ãããŠïŒmlã®ã¢
ã³ãã«ã«å å¡«ãããããã·ãŒã«ããŠ20åé121â
ã§ãªãŒãã¯ã¬ãŒãã«ããããåã¢ã³ãã«ã¯mlåœã
æ°èŠååç©(a)10mgãå«ãã 次ã®å®æœäŸã¯æ¬çºæã®ååç©ãæŽã«äŸç€ºããã å®æœäŸ ïŒ ïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãžã¢ãã³
ãžãããã¯ãã©ã€ã 500mlã®ããã©ããããã©ã³äžã®21.5ïœ
ïŒ0.1MïŒã®ïŒâããªã¡ãã«ã·ãªã«ãããâïŒâã€
ãã«âïŒâã€ãããã³ãžã«ã®â70âã®æº¶æ¶²ã66.5
mlã®ïœâããã«ãªããŠã ã®1.5M溶液ã§åŠçããã
â70âã«æŒããŠïŒåéã®åŸã100mlã®ããã©ãã
ããã©ã³äžã®8.0ïœã®äºéãš25.4ïœã®ãšãŠçŽ ãã
ã€ãããããšãŠåäºéã®æº¶æ¶²ãå ãããããçã
ã溶液ã¯â70âã«æŒããŠ20åéä¿ããããã®åŸ
5.6ïœïŒ0.1MïŒ6.65mlïŒã®ïŒâãããããŒã«ãâ
70âã§æ»ŽäžããŠå ããããã溶液ãâ70âã§30å
éä¿æããã次ã«7.8ïœïŒ0.1MïŒ70mlïŒã®å¡©åã¢
ã»ãã«ãå ããããã溶液ã宀枩ãŸã§æž©ãŸããã
ã«ãããšãŒãã«ã§åžéãéçé žãããªãŠã 氎溶液
ã§è¯ãæŽãã次ã«å¡©åãããªãŠã 氎溶液ã§æŽãã
ç¡«é žãã°ãã·ãŠã äžã§ä¹Ÿç¥ããŠèžçºããŠæ²¹ãæ®
ããããã200mlã®ã€ãœãããã«ã¢ã«ã³ãŒã«äžã§
åãããã10ïœïŒ0.093MïŒã®ããšãã«ããã©ãž
ã³ã§åŠçãããæ··åç©ãéæµãããªãã20åéå
ç±ããŠæ¬¡ã«æº¶åªãèžçºãããæ®æž£ã¯ã¯ãããã«ã
äžã«æº¶è§£ããã¯ãããã«ã ã§å å¡«ãããäºé žåã·
ãªã³ã³ã®ã«ã©ã ã«ããããããã¯ãããã«ã ã§æ¬¡
ã«ïŒïŒ ã¡ã¿ããŒã«ïŒã¯ãããã«ã ã§æº¶åºããŠïŒâ
ããªã¡ãã«ã·ãªã«ã¢ã»ãã¬ã³âïŒâã¢ããããâ
ïŒâãšã³âïŒâãªãŒã«ã®ã¢ã»ãã¢ãããåŸããã
ã30mlã®ãšã¿ããŒã«äžã«æº¶è§£ããŠ30mlã®æ°Žäžã®
2.5ïœã®æ°Žé žåã«ãªãŠã ã§å®€æž©ã«æŒããŠåŠçãã
ãããåŸã«ã¡ã¿ããŒã«ãæ¿Ÿå¥ãããæ°Žæ§æ®æž£ã¯å¡©
åãããªãŠã ã§é£œåããå¡©åã¡ãã¬ã³ã§è¯ãæœåº
ããããææ©å±€ã¯ç¡«é žãã°ãã·ãŠã äžã§ä¹Ÿç¥ãã
æ¿çž®ãããŠæ®æž£ãæ®ãããããã¯ãããã«ã ïŒç³
æ²¹ãšãŒãã«ã§åçµæ¶ã«ãããŠïŒâã¢ãããããµâ
ïŒâãšã³âïŒâã€ã³âïŒâãªãŒã«ïŒèç¹94âïŒã®
ã¢ã»ãã¢ãããåŸãããã®994mgïŒ6.5mMïŒã15
mlã®ããã©ããããã©ã³äžã«åããããŠæ°Žé žåã
ããªãŠã ã®50ïŒ æžæ¿æ¶²ïŒ0.5mMïŒ24mgã«å ããã
çŽ25âã«æŒããŠïŒååŸã溶液ã泚å°åšãã滎äžã
ãŠäºãâ23âã«å·ããããïŒãã©ã€ã¢ã€ã¹ïŒåå¡©
åççŽ ïŒ30mlã®ããã©ããããã©ã³äžã®935mg
ïŒ6.5mMïŒã®ããªã¯ããã¢ã»ããããªã«ã®æº¶æ¶²ã«
å ãããçãã溶液ã¯1.5æéâ23âã§æ¹æãã
ãŠã次ãã§çŽ25âã§èžçºãããŠæ²¹ãæ®ããããã
30mlã®ãã·ã¬ã³äžã«æº¶è§£ããŠéæµäžã«ïŒæéå ç±
ã次ã«çŽ25âã§äžå€æŸçœ®ãããçããæ²æŸ±ã¯éã
ãããã¯ãããã«ã ã§åçµæ¶ã6N HCl 40mlãš
ã¡ã¿ããŒã«100mlãšã«äžç·ã«ãããã溶液ã¯éæµ
äžã«12æéå ç±ããã次ã«æ¿çž®ããããçããæ®
枣ã¯ã¯ãããã«ã ã§è¯ãæŽããæšçã§åŠçãæ¿Ÿé
ããŠèžçºããŠæ®æž£ãæ®ããããããšã¿ããŒã«ã§å
çµæ¶ããŠïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãž
ã¢ãã³ãžãããã¯ãã©ã€ããèç¹175âïŒå解ïŒ
ãåŸãã å®æœäŸ ïŒ ïŒïŒïŒâãããâïŒâãšã³âïŒâã€ã³ãžã¢ãã³ 500mlã®ã¢ã³ã¢ãã¢äžã®2.3ïœã®ïŒ0.1MïŒãã
ãªãŠã ããé ããããããªãŠã ã¢ã»ããªãã®æº¶æ¶²
ã«ã35ïœïŒ35mMïŒã®ïŒâããããã·ãã³ãâïŒ
âãšããŒã«ãå ãããããäžæéåŸã«å¡©åã¢ã³ã¢
ããŠã ãå ããããã¢ã³ã¢ãã¢ã¯èžçºããããã«
ããããæ®æž£ã¯ãšãŒãã«äžã«ãšããããããæ¿Ÿé
ãããŠæ¿çž®ãããæ®æž£ãæ®ããããã200mlã®ã
ãã©ããããã©ã³äžã«ãšããããŠ48æéã25âã§
18.3ïœã®ïŒ70mMïŒããªããšãã«ãã¹ãã€ã³ã
12.1ïœïŒ70mMïŒã®ãžãšãã«ã¢ãŸãžã«ã«ããã·ã¬
ãŒãåã³10.2ïŒ70mMïŒã®ãã¿ã«ã€ãããšå ±ã«æ¹
æãããçããæ²æŸ±ãæ¿Ÿå»ããã¡ã¿ããŒã«ã§åçµ
æ¶ãã次ã«30mlã®ãšã¿ããŒã«äžã«æº¶è§£ããããšã¿
ããŒã«æº¶æ¶²ã¯ããã©ãžã³æ°Žåç©ïŒ1.74ïœïŒã§éæµ
äžã«äžå€åŠçãããã®åŸæº¶åªãèžçºããæ®æž£ãïŒ
ïŒ æ°Žé žåã«ãªã§å¡©åºã«ãŸã§åŠçãããžã¯ããã¡ã¿
ã³ã§æœåºããèžçºããŠèžçããŠïŒïŒïŒâãããâ
ïŒâãšã³âïŒâã€ã³ãžã¢ãã³ãåŸãã å®æœäŸïŒã®æé ã«æŒããŠïŒâãããããŒã«ãé©
åœéã®ïŒâããããŒã«ã«ããããšãã«ãïŒïŒïŒâ
ãããâïŒâãšã³âïŒâã€ã³ãžã¢ãã³äºå¡©é žå¡©ã
åŸãããã ODCã®äžå¯éçé»å®³ JACS100ã2551ã2553é ïŒ1978ïŒã«èšèŒãã
ãæ¹æ³ã§ãã©ã³ã¹ïŒïŒïŒâããã¹âïŒâãšã³âïŒ
âã€ã³ãžã¢ãã³ã®ã©ããèèãªã«ããã³ãã«ã«ã
ãã·ã©ãŒãŒäžæŽ»æ§åé床å®æ°ïŒKinactïŒã2.3Ã
10-3ã§ãã€ãããã®ããã«æ¬çºæã®ååç©ã¯
ODCäœçšãæããåŸã€ãŠæè «çãåã³å¢èïŒä¿
é²ïŒè¬æçµçšéã«å¯Ÿããæçšæ§ãæ¯æãããã
Claims (1)
- ãç¹èš±è«æ±ã®ç¯å²ã ïŒ åŒ ã®ååç©ãåã³è£œè¬åŠçã«åãå ¥ããããå¡©ãã
ãã³ãããã®åã ã®å åŠç°æ§äœé¡ïŒäœããåŒäžïŒ¡
ã¯ã¡ãã¬ã³ããšãã¬ã³åã¯ãšããªãã³ã§ããïŒã ïŒ ïŒïŒïŒâããã¹âïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³åã¯ãã®è£œè¬åŠçã«åãå ¥ããããå¡©ã§ããç¹
èš±è«æ±ã®ç¯å²ç¬¬ïŒé ã«èšèŒã®ååç©ã ïŒ ïŒïŒïŒâãããâïŒâãšã³âïŒâã€ã³ãžã¢ã
ã³åã¯ãã®è£œè¬åŠçã«åãå ¥ããããå¡©ã§ããç¹
èš±è«æ±ã®ç¯å²ç¬¬ïŒé ã«èšèŒã®ååç©ã ïŒ åŒ ã®ååç©ãåã³è£œè¬åŠçã«åãå ¥ããããå¡©ãã
ãã³ãããã®åã ã®å åŠç°æ§äœé¡ïŒäœããåŒäžïŒ¡
ã¯ã¡ãã¬ã³åã¯ãšããªãã³ã§ããïŒã補é ããæ¹
æ³ã«æŒããŠã ä»»æä»å çã«ïŒäŸ¡éå±éœã€ãªã³ã®ååšäžã«åã¯
éååšäžã«ãé©åœã«ä¿è·ããããããã®ã«ã¢ãã³
èªå°äœïŒåœéãé©åœãªåŒ·å¡©åºã§åŠçããçæãã
ä¿è·ããããããã®ã«ã¢ãã³ã«ã«ãããªã³äžéäœ
ãïŒâãããããŒã«åã¯ïŒâããããŒã«ã§ã¢ã«ã
ã«åããã¢ã«ãã«åãããèªå°äœãé©åœãªããã²
ã³åç©ãäœçŽã¢ã«ãã«ãããã«ã¡ãŒããåã¯ç¬¬äž
ãããã·ã«ã«ããã«ã¢ãžãã§ã¢ã·ã«åãã次ãã§
å æ°Žå解ããŠãã¢ããåã¯ã«ã«ãã¡ãŒããåŸãã
ããé©åœãªå¡©åºã§åŠçããŠã«ã«ãããµãããåŸ
ãŠããããé©åœãªæº¶åªã§è§Šåªéã®å¡©åºã®ååšäžã§
çŽâ30ãïŒâã«æŒããŠçŽ30åãïŒæéããªã¯ãã
ã¢ã»ããããªã«ã§åŠçããŠããªã¯ããã¡ãã«ã€ã
ããŒããšã¹ãã«ãåŸãŠããããé極æ§æº¶åªäžã§çŽ
110âã140âã«æŒããŠçŽïŒã10æéå ç±ããŠããª
ã¯ããã¡ãã«ã¢ã»ãã¢ãããåŸãŠããããæ°Žæ§ã®
é žåã¯å¡©åºã§å æ°Žå解ããäœããã®å Žåãäžèšã¢
ã«ãã«ååã³ã¢ã·ã«ååå¿ã¯äžæ§æº¶åªäžã«æŒããŠ
çŽâ125âã25âã§çŽ30åã24æéå®æœããããš
ãããªãæ¹æ³ã
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US81211577A | 1977-07-01 | 1977-07-01 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5481205A JPS5481205A (en) | 1979-06-28 |
| JPS635384B2 true JPS635384B2 (ja) | 1988-02-03 |
Family
ID=25208552
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP7927178A Granted JPS5481205A (en) | 1977-07-01 | 1978-07-01 | Amine and amino acid derivatives |
Country Status (7)
| Country | Link |
|---|---|
| JP (1) | JPS5481205A (ja) |
| BE (1) | BE868591A (ja) |
| CA (1) | CA1121375A (ja) |
| DE (1) | DE2827759A1 (ja) |
| FR (1) | FR2395982A1 (ja) |
| GB (1) | GB2001059B (ja) |
| ZA (1) | ZA783274B (ja) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ197394A (en) * | 1980-06-16 | 1984-09-28 | Merrell Dow Pharma | Inhibition of protozoal growth in animals with certain-substituted-amines or amino acids |
| US4437873A (en) | 1981-03-23 | 1984-03-20 | Merrell Dow Pharmaceuticals Inc. | Method of inhibiting algae |
| DE3207787A1 (de) * | 1982-03-04 | 1983-09-08 | Robert Bosch Gmbh, 7000 Stuttgart | Kraftstoffzumesssystem fuer eine brennkraftmaschine |
| US5013719A (en) * | 1988-05-13 | 1991-05-07 | Merrell Dow Pharmaceuticals Inc. | Method of effecting immunosuppression |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2766285A (en) * | 1952-10-20 | 1956-10-09 | Lilly Co Eli | Substituted aminopropynes and process for their preparation |
| US3079345A (en) * | 1959-04-30 | 1963-02-26 | Dow Chemical Co | Propargyl compounds as corrosion inhibitors |
| US3959356A (en) * | 1975-03-18 | 1976-05-25 | Richardson-Merrell Inc. | Acetylene derivatives of amino acids |
| US3960927A (en) * | 1975-03-18 | 1976-06-01 | Richardson-Merrell Inc. | Olefinic derivatives of amino acids |
-
1978
- 1978-06-06 CA CA000304899A patent/CA1121375A/en not_active Expired
- 1978-06-07 ZA ZA00783274A patent/ZA783274B/xx unknown
- 1978-06-24 DE DE19782827759 patent/DE2827759A1/de not_active Withdrawn
- 1978-06-27 GB GB7827972A patent/GB2001059B/en not_active Expired
- 1978-06-28 FR FR7819351A patent/FR2395982A1/fr active Granted
- 1978-06-29 BE BE188951A patent/BE868591A/xx not_active IP Right Cessation
- 1978-07-01 JP JP7927178A patent/JPS5481205A/ja active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| GB2001059B (en) | 1982-04-21 |
| ZA783274B (en) | 1979-06-27 |
| FR2395982A1 (fr) | 1979-01-26 |
| BE868591A (fr) | 1978-10-16 |
| DE2827759A1 (de) | 1979-01-25 |
| GB2001059A (en) | 1979-01-24 |
| FR2395982B1 (ja) | 1980-07-18 |
| JPS5481205A (en) | 1979-06-28 |
| CA1121375A (en) | 1982-04-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US4134918A (en) | Alpha-halomethyl derivatives of amines | |
| US4423044A (en) | 3,4-Dihydro-5H-2,3-benzodiazepine derivatives and pharmaceutical use thereof | |
| US4330559A (en) | Method of treating benign prostatic hypertrophy | |
| KR880002310B1 (ko) | íìíì¬ ì믌ë¥ì ì ì¡°ë°©ë² | |
| GB2150932A (en) | Indoles | |
| US4139563A (en) | α-ACETYLENIC DERIVATIVES OF AMINES | |
| US4413141A (en) | 2-(Difluoromethyl)-2,5-diaminopentanoic acid | |
| US4309442A (en) | Method for controlling fertility in mammals | |
| US4326071A (en) | Halomethyl derivatives of gamma-aminobutyric acid and related compounds | |
| CA1091661A (en) | .alpha.-HALOMETHYL DERIVATIVES OF .alpha.-AMINO ACIDS | |
| US5614557A (en) | Method of controlling tumor growth rate | |
| US4182891A (en) | α-Acetylenic derivatives of α-amino acids | |
| Huebner et al. | N-methyl-N-2-propynyl-1-indanamine. A potent monoamine oxidase inhibitor | |
| US3622675A (en) | Anorexigenic composition and method | |
| JPS635384B2 (ja) | ||
| US4180509A (en) | α-Ethynyl tryptophanes | |
| US4267374A (en) | Derivatives of amines and amino acids | |
| US4323704A (en) | αAcetylene and α-vinyl derivatives of amino acids | |
| US4560795A (en) | α-Halomethyl derivatives of α-amino acids | |
| EP0000355B1 (en) | New indole derivatives, processes for their preparation, and pharmaceutical compositions containing them. | |
| US4147873A (en) | α-Vinyl derivatives of α-amino acids | |
| US4183858A (en) | α-Vinyl tryptophanes | |
| CA1157030A (en) | .alpha.-VINYL AMINO ACIDS | |
| JPS6326101B2 (ja) | ||
| US4260823A (en) | α-Acetylenic derivatives of α-amino acids |