Buprenorphine is a potent kappa-opioid receptor antagonist in pigeons and mice

Eur J Pharmacol. 1988 Jul 14;151(3):457-61. doi: 10.1016/0014-2999(88)90543-2.


Buprenorphine was studied for its antagonist activity against the specific kappa-opioid agonist U-50,488H in pigeons responding under a multiple schedule of grain presentation and in mice in an antinociception test. U-50,488H decreased rates of responding of pigeons over the dose range (2.5-20 mg/kg i.m.). In the presence of 0.32 mg/kg of buprenorphine, the U-50,488H dose-effect curve was shifted to the right approximately two-fold. Buprenorphine alone (0.01-0.08 mg/kg s.c.) inhibited in mice the abdominal stretching induced by i.p. acetic acid. beta-Funaltrexamine pretreatment blocked the mu-like agonist analgesic effect of buprenorphine and revealed an antagonist action of buprenorphine against 2.5 mg/kg of U-50,488H over the same dose range that it produced antinociception at the mu-receptor. Thus, buprenorphine is a potent kappa-opioid receptor antagonist, producing the kappa-antagonist activity over the same dose range that it produces its mu-mediated partial agonist activity.

MeSH terms

  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • Analgesics / pharmacology
  • Animals
  • Buprenorphine / pharmacology*
  • Columbidae
  • Male
  • Mice
  • Muscle Contraction / drug effects
  • Naltrexone / analogs & derivatives
  • Naltrexone / pharmacology
  • Narcotic Antagonists*
  • Pyrrolidines / pharmacology
  • Receptors, Opioid / metabolism*
  • Receptors, Opioid, kappa
  • Reinforcement Schedule


  • Analgesics
  • Narcotic Antagonists
  • Pyrrolidines
  • Receptors, Opioid
  • Receptors, Opioid, kappa
  • Buprenorphine
  • Naltrexone
  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • beta-funaltrexamine