TH2785A - GRF analogues - Google Patents

Abstract

Human GRF (hGRF), rat GRF (rGRF), porcine GRF (pGRF), and bovine GRF (bGRF) have been studied and synthesized. This invention demonstrates the synthesis of a potent peptide that stimulates pituitary GH secretion in animals, including humans. This synthetic peptide is resistant to enzymatic degradation in the body and has the following sequence (formula), where (formula) with substitutions (formula) or without substitutions (formula) are natural amino acids. In addition, peptides with some radicals or radicals between R28 and R44 missing are obtained, and peptides where R2 is D-NMA and/or R14 is D-Leu and/or R29 is D-Arg are obtained. These peptides, along with their salts, may be used in diagnostic purposes.

Claims (20)

1. Synthetic peptides or their non-toxic salts have a sequence (formula) where (formula) is substituted (formula) or unsubstituted (formula) is a natural amino acid. Additionally, they yield peptides with some or all radicals between R28 and R44 missing, and peptides where R2 is D-NMA and/or R14 is D-Leu and/or R29 is D-Arg. 2. The peptide of claim 1 at R2 is D-NMA. 3. The peptide of claim 1 at R29 is D-Arg. 4. The peptide of claim 1 at R14 is D-Leu. 5. The peptide of claim 1 at R25 is D-Glu. 6. The peptide of claim 1 at R27 is Nle. 7. The peptide of claim 1 at R17 is D-Leu. 8. The peptide of claim 1 at R25 is D-Asp. 9. The peptide of claim 1 at R1 is (formula). Radicals 30 through 44 are omitted. 10. The peptide of claim 9 at R17 is (formula). 11. The peptide of claim 2 at R3 is (formula). 12. The peptide of claim 11 at R17 is (formula). Radicals 30 to 44 have been omitted. 13. The peptide of the second claim at R14 is D-Leu. 14. The peptide of claim 2 at R29 is D-Arg. 15. A pharmaceutical compound that stimulates GH secretion in animals, consisting of the peptide of claim I or its non-toxic salts in an effective dose, and its liquid or solid carrier, which is pharmaceutically or veterinarily acceptable. 16. A method for the treatment of a person, consisting of administering a mixture of the claims of Patent 15 in an effective dose. 17. A method to stimulate the secretion of growth hormone in animals involves administering synthetic peptides or their non-toxic salts to the animal in quantities that produce a sequence of (formula), where R1 is (formula) which is replaced by (formula) or not replaced by (formula) is a natural amino acid, where any or all radicals between R28 and R44 may be omitted and R2 is D-NMA, or R4 is D-Leu, or R29 is D-Arg. 18. Methods for supporting the growth of non-human warm-blooded animals as per claim 17. 19. Methods for supporting the growth of by administering to fish or cold-blooded animals as per claim 17. 20. Methods for accelerating the growth of non-human animals by administering synthetic peptides in the following sequence, in effective amounts (formula), where R1 is (formula) replaced by (formula) or its non-toxic salt (20 claims, 4 pages, 0 images).