Synthetic peptides related to the dermorphins. II. Synthesis and biological activities of new analogues.
A new series of analogues of the potent opiate-like peptides dermorphins (mainly tetra- and pentapeptides) were synthesized in order to better evaluate the structure-activity relationships. Relative potencies were referred to dermorphin (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2), the prototype of this class of frog skin peptides. Peripheral opioid activity (guinea-pig ileum and mouse vas deferens) was determined for all the dermorphin analogues. For a selected number of them also central analgesic (hot plate and tail-flick tests) and cataleptic activities were assayed in the rat by intracerebroventricular administration.
D000698:Analgesia; D000818:Animals; D001681:Biological Assay; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D008297:Male; D051379:Mice; D009294:Narcotics / Q000138:chemical synthesis* / Q000494:pharmacology; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D018847:Opioid Peptides; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000187:drug effects
D009294:Narcotics; D009842:Oligopeptides; D018847:Opioid Peptides; C030058:dermorphin