NOVEL GH-RH ANALOGS WITH POTENT AGONISTIC EFFECTS

摘要

There are provided a novel series of peptide analogs of hGH-RH(1-29)NH2 and hGH-RH(1-30)NH2 which show high activities in stimulating the release of pituitary GH in animals. They retain their physiological activity in solution for extended periods of time and resist enzymic degradation in the body. These novel and useful properties appear to be due to novel substitution patterns ant at the 1, 15, 27 and 29 positions on the peptide.

主权项

1. A GH-RH agonist peptide having the formula:
[R1-A1, A2, A6, A8, A11, A12, A15, A20, A21, A22, Nle27, A28, Agm29]hGH-RH(1-29)NH2, wherein R1 is Ac, Tfa, or is absent, A1 is Tyr, Dat, or N-Me-Tyr, A2 is Ala, D-Ala, Abu, or D-Abu, A6 is Phe or Fpa5, A8 is Asn, Ala, Gln, Thr, or N-Me-Ala, A11 is Arg, His, or Har, A12 is Orn, or Lys(Me)2, A15 is His, Abu, Aib, Aah, Aap, Ala, or D-Ala A20 is Arg, His, or Har, A21 is Orn, or Lys(Me)2, A22 is Leu, or Orn, A28 is Ser, or Asp, and pharmaceutically acceptable salts thereof.