Buprenorphine has potent kappa opioid receptor antagonist activity

Neuropharmacology. 1987 Sep;26(9):1445-7. doi: 10.1016/0028-3908(87)90112-2.

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.

MeSH terms

  • Animals
  • Benzomorphans / pharmacology
  • Buprenorphine / pharmacology*
  • Diuresis / drug effects
  • Drug Combinations
  • Male
  • Naltrexone / analogs & derivatives
  • Naltrexone / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / classification
  • Receptors, Opioid / drug effects*

Substances

  • Benzomorphans
  • Drug Combinations
  • Receptors, Opioid
  • Buprenorphine
  • Naltrexone
  • beta-funaltrexamine
  • bremazocine