title: Buprenorphine has potent kappa opioid receptor antagonist activity.
abstract: Buprenorphine was studied for its effects on urinary output to determine if it was an agonist, partial agonist, or antagonist at the kappa receptor. Buprenorphine was a potent antagonist of bremazocine-induced urination and had no kappa agonist activity. Thus, the high affinity that buprenorphine has for the kappa receptor results in potent kappa receptor antagonist activity in vivo.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285.
authors.forename: J D
authors.initials: JD
authors.lastname: Leander
mesh_terms: D000818:Animals; D001575:Benzomorphans / Q000494:pharmacology; D002047:Buprenorphine / Q000494:pharmacology*; D004231:Diuresis / Q000187:drug effects; D004338:Drug Combinations; D008297:Male; D009271:Naltrexone / Q000031:analogs & derivatives / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000145:classification / Q000187:drug effects*
chemical_list: D001575:Benzomorphans; D004338:Drug Combinations; D011957:Receptors, Opioid; D002047:Buprenorphine; D009271:Naltrexone; C024524:beta-funaltrexamine; C027248:bremazocine