title: The analgesic activity of biphalin and its analog AM 94 in rats.
abstract: Biphalin is an opioid linear octapeptide, which displays a broad affinity for all opioid receptors (μ, δ and κ), as well as exceptionally high antinociceptive activity. AM 94 is a biphalin analog and a selective agonist at μ and δ opioid receptors. This study investigated the antinociceptive profile of AM 94. All antinociception evaluations were made in adult male rats using the hot-plate test. AM 94 proved to induce greater and longer antinociception compared to biphalin following intracebroventricular (1 nmol/kg) and intravenous administration (1200 nmol/kg) as evaluated by % maximum possible effect (M.P.E.), when administered intracerebroventricularly and intravenously and sustained analgesia up to 210 min. The antinociceptive activities of biphalin and AM 94 were antagonized by naloxone (10mg/kg intraperitoneally). Our data suggest that AM 94 could be regarded as a novel pharmacologically active opioid compound for eliciting potent and sustained analgesia after central and peripheral administration.
authors.affiliation: Department of Drug Sciences, G. d'Annunzio University, via dei Vestini 31, 66013 Chieti, Italy.
authors.forename: Sheila
authors.initials: S
authors.lastname: Leone
authors.forename: Annalisa
authors.initials: A
authors.lastname: Chiavaroli
authors.forename: Giustino
authors.initials: G
authors.lastname: Orlando
authors.forename: Adriano
authors.initials: A
authors.lastname: Mollica
authors.forename: Chiara
authors.initials: C
authors.lastname: Di Nisio
authors.forename: Luigi
authors.initials: L
authors.lastname: Brunetti
authors.forename: Michele
authors.initials: M
authors.lastname: Vacca
mesh_terms: D000700:Analgesics / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D004195:Disease Models, Animal; D004745:Enkephalins / Q000008:administration & dosage / Q000494:pharmacology*; D007275:Injections, Intravenous; D007276:Injections, Intraventricular; D008297:Male; D009270:Naloxone / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology; D009842:Oligopeptides / Q000008:administration & dosage / Q000494:pharmacology*; D010146:Pain / Q000188:drug therapy*; D010879:Piperazines / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013997:Time Factors
chemical_list: C575160:(Tyr-Ala-Gly-pF-Phe)2-piperazine; D000700:Analgesics; D004745:Enkephalins; D009292:Narcotic Antagonists; D009842:Oligopeptides; D010879:Piperazines; D009270:Naloxone; C053673:biphalin