Profile of activity of kappa receptor agonists in the rabbit vas deferens

Eur J Pharmacol. 1985 Apr 16;110(3):317-22. doi: 10.1016/0014-2999(85)90558-8.

Abstract

The purpose of this study was to investigate further the kappa opioid receptor selectivity of the field-stimulated isolated rabbit vas deferens preparation and to study the profile of a series of kappa agonists in this tissue. Agonists acting at mu, delta and sigma receptors were without detectable effect in the rabbit vas deferens. But a number of kappa agonists, including bremazocine, tifluadom, ethylketocyclazocine, ketocyclazocine, U-50,488 and Win 42,610 all depressed contractions, producing parallel dose-response curves. Mr 2034 generally produced a shallower dose-response curve and achieved a lower maximum effect, thus acting like a partial agonist. The effect of ethylketocyclazocine was not reduced by the irreversible mu antagonist, beta-funaltrexamine, confirming that it is not acting via mu receptors. Another group of drugs, including nalorphine, butorphanol and proxorphan, which produce an agonist action via kappa receptors in the guinea-pig ileum and mouse vas deferens, were antagonists in the rabbit vas deferens, suggesting that this tissue will only respond to high efficacy kappa agonists.

MeSH terms

  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • Analgesics / pharmacology
  • Animals
  • Benzodiazepines / pharmacology
  • Benzomorphans / pharmacology
  • Butorphanol / pharmacology
  • Cyclazocine / analogs & derivatives
  • Cyclazocine / pharmacology
  • Ethylketocyclazocine
  • In Vitro Techniques
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects*
  • Nalorphine / pharmacology
  • Naloxone / pharmacology
  • Pyrrolidines / pharmacology
  • Rabbits
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / physiology*
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu
  • Vas Deferens / drug effects

Substances

  • Analgesics
  • Benzomorphans
  • Pyrrolidines
  • Receptors, Opioid
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu
  • Benzodiazepines
  • Naloxone
  • Ethylketocyclazocine
  • 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
  • ketazocine
  • bremazocine
  • Cyclazocine
  • Butorphanol
  • tifluadom
  • Nalorphine