PMID: 8614238Mar 3, 1995Paper

Buprenorphine exerts its antinociceptive activity via mu 1-opioid receptors

Life Sciences
J KameiY Kasuya

Abstract

The mechanism of the antinociceptive effect of buprenorphine was assessed by administering selective mu-, mu1--, delta- and kappa-opioid receptor antagonists in mice. Intraperitoneal administration of buprenorphine, at doses of 0.3 to 3 mg/kg, produced dose-dependent antinociception in the tail-flick test. The antinociceptive activity of buprenorphine did not result from the activation of kappa- or delta-opioid receptors, since treatment with either nor-binaltorphimine, a selective kappa-opioid receptor antagonist, or naltrindole, a selective delta-opioid receptor antagonist, was completely ineffective in blocking buprenorphine-induced antinociception. However, the antinociceptive effect of buprenorphine was significantly antagonized by beta-funaltrexamine, a selective mu-opioid receptor antagonist. Moreover, selective mu1-opioid receptor antagonist, naloxonazine and naltrexonazine, also significantly antagonized the antinociceptive effect of buprenorphine. Co-administration of kappa- and delta-opioid receptor antagonist with the mu-opioid receptor antagonists had no significant effect on the antagonistic profiles of the mu-opioid receptor antagonists on the antinociceptive effect of buprenorphine. These results suggest that bu...Continue Reading

Citations

May 2, 2003·The Journal of Pharmacology and Experimental Therapeutics·Hirokazu MizoguchiLeon F Tseng
Jun 14, 2013·Laboratory Animals·Larry G ThaeteAndrew T Dudley
Oct 1, 2013·Pharmacological Reviews·Gavril W Pasternak, Ying-Xian Pan
Sep 6, 2005·European Journal of Pain : EJP·Babette KögelElmar Friderichs
Feb 11, 2014·Anesthesiology·Kelly Yan ChenJianren Mao
Apr 22, 2004·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Soichiro IdeKazutaka Ikeda
Apr 25, 2020·Pain Medicine : the Official Journal of the American Academy of Pain Medicine·Asimina LazaridouChristopher Gilligan

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