Pharmacological characterization in vivo of the novel opiate, beta-funaltrexamine.
The profile of action of beta-funaltrexamine (beta-FNA), the fumaramate methyl ester derivative of naltrexone, on antinociceptive tests in vivo was investigated. Beta-FNA demonstrated antinociceptive actions that were of short duration and that appeared to be mediated by kappa receptor interaction. In contrast, the antagonist actions of beta-FNA were of remarkably long duration and were selective toward nu agonist interactions. This profile of action is consistent with the profile of action of beta-FNA in vitro. The selective long-lasting antagonism of mu-mediated effects by beta-FNA may be of great value in the elucidation of multiple opioid receptor function.
D000085:Acetates; D019342:Acetic Acid; D000701:Analgesics, Opioid; D000818:Animals; D004347:Drug Interactions; D005260:Female; D008297:Male; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009269:Nalorphine / Q000494:pharmacology; D009270:Naloxone / Q000031:analogs & derivatives*; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009294:Narcotics / Q000494:pharmacology*; D010146:Pain / Q000139:chemically induced / Q000503:physiopathology; D011930:Reaction Time / Q000187:drug effects
D000085:Acetates; D000701:Analgesics, Opioid; D009294:Narcotics; D009270:Naloxone; D009271:Naltrexone; C024524:beta-funaltrexamine; D009020:Morphine; D019342:Acetic Acid; D009269:Nalorphine