Further evidence for the existence of a homogenous beta-endorphin-sensitive receptor population in the rat tail artery

Eur J Pharmacol. 1988 Mar 1;147(2):305-8. doi: 10.1016/0014-2999(88)90793-5.

Abstract

Isolated rat tail arteries were perfused and vasoconstriction was evoked by electrical field stimulation (2 pulses at 1 Hz every 2 min). The vasoconstriction was depressed by DAGO (IC50 = 611 nM) and beta-endorphin (IC50 = 37 nM). Structuraly analogues and shorter fragments of beta-endorphin were also tested. beta-Endorphin and beta-endorphin-(1-26) were about equipotent whereas the beta-endorphin fragments 1-17, 1-16 and 6-31 were inactive. The potencies of beta-endorphin, beta-endorphin-(1-26), -(1-17) and -(1-16) were not changed in the presence of peptidase inhibitors. Structural analogues such as [D-Ala2]beta-endorphin or [Leu5]beta-endorphin had a somewhat lower potency than beta-endorphin itself. Naloxone 30 nM antagonized the effects of DAGO and beta-endorphin to a similar extent with dissociation constants 3.8 and 3.7 nM, respectively for the antagonist against the agonists. The results support the existence in the rat tail artery of a homogenous population of beta-endorphin-sensitive receptors which may belong to the epsilon-type.

MeSH terms

  • Animals
  • Electric Stimulation
  • Endorphins / pharmacology
  • In Vitro Techniques
  • Male
  • Muscle, Smooth, Vascular / drug effects*
  • Protease Inhibitors / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / metabolism*
  • Regional Blood Flow / drug effects
  • Tail / blood supply
  • Vasoconstriction / drug effects
  • beta-Endorphin / metabolism*
  • beta-Endorphin / pharmacology

Substances

  • Endorphins
  • Protease Inhibitors
  • Receptors, Opioid
  • beta-Endorphin