Opioid peptide. Structure-activity relationships in dermorphin tetrapeptide-amides. II.
Preliminary pharmacological data and the characterization of sixteen synthetic tetrapeptide-amide analogs of dermorphin (opioid heptapeptide) are reported. N,N-dialkylamides displayed reduced or no activity; on the contrary, derivatization of H-Tyr-D-Ala-Phe-Gly-OH C-terminus by suitable amide moieties (1-adamantanamine, 1-adamantane-methylamino, or D-alpha-methylbenzylamine) produced potent analogues with peripheral and central opioid activities comparable to, or higher than those of dermorphins.
D000700:Analgesics; D000818:Animals; D004723:Endorphins / Q000494:pharmacology*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009126:Muscle Relaxation / Q000187:drug effects; D009270:Naloxone / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology; D018847:Opioid Peptides; D013329:Structure-Activity Relationship
D000700:Analgesics; D004723:Endorphins; D009842:Oligopeptides; D018847:Opioid Peptides; C030058:dermorphin; D009270:Naloxone