Classification of presynaptic opioid receptors in the rabbit ear artery by competitive antagonists

Eur J Pharmacol. 1986 Mar 11;122(1):153-6. doi: 10.1016/0014-2999(86)90173-1.

Abstract

Electrical field stimulation (5 impulses at 5 Hz every min) evoked vasoconstriction in the rabbit isolated ear artery. The vasoconstriction was depressed by [Leu5]enkephalin (IC50 = 47 nM) and ethylketocyclazocine (IC50 = 80 nM). Naloxone 300 nM antagonized the effect of both agonists with a similar potency; the respective KB values were 41 and 64 nM. ICI 174864 1000 nM antagonized only the effect of [Leu5]enkephalin (KB = 126 nM) but not that of ethylketocyclazocine. In contrast, MR 2266 100 nM was a more potent antagonist of ethylketocyclazocine (KB = 8 nM) than of [Leu5]enkephalin (KB = 45 nM). The results suggest that the rabbit ear artery contains both presynaptic delta- and kappa-receptors.

MeSH terms

  • Animals
  • Arteries / innervation*
  • Benzomorphans / metabolism
  • Binding, Competitive
  • Biological Assay
  • Cyclazocine / analogs & derivatives
  • Cyclazocine / metabolism
  • Ear / blood supply
  • Enkephalin, Leucine / analogs & derivatives
  • Enkephalin, Leucine / metabolism
  • Ethylketocyclazocine
  • In Vitro Techniques
  • Naloxone / metabolism
  • Rabbits
  • Receptors, Opioid / classification*
  • Receptors, Opioid / metabolism
  • Synaptic Membranes / metabolism

Substances

  • Benzomorphans
  • Receptors, Opioid
  • Naloxone
  • MR 2266
  • Ethylketocyclazocine
  • Enkephalin, Leucine
  • N,N-diallyl-tyrosyl-alpha-aminoisobutyric acid-phenylalanyl-leucine
  • Cyclazocine