Structure-activity relationships for dermorphin-related tetrapeptides.
The opiate-like activity of six newly synthesized dermorphin-related tetrapeptides was determined in guinea pig ileum, mouse vas deferens and mouse tail-flick tests. Naloxone was a powerful antagonist of all compounds. Moreover, the biological activities of the compounds under examination were correlated in a statistically significant way to the lipophilic character of the C-terminal substituents and to an indicator variable taking into account the presence of an amidic group at the C-terminus.
D000818:Animals; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006168:Guinea Pigs; D007082:Ileum; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects; D009294:Narcotics / Q000494:pharmacology*; D009842:Oligopeptides / Q000494:pharmacology*; D018847:Opioid Peptides; D011930:Reaction Time / Q000187:drug effects; D013329:Structure-Activity Relationship; D013623:Tail; D014649:Vas Deferens
D009294:Narcotics; D009842:Oligopeptides; D018847:Opioid Peptides; C030058:dermorphin