Evidence that dynorphin-(1-13) acts as an agonist on opioid kappa-receptors

Eur J Pharmacol. 1982 Jan 22;77(2-3):137-41. doi: 10.1016/0014-2999(82)90008-5.

Abstract

The study concerned the opioid-receptor subtype on which dynorphin-(1-13) acts in in vitro isolated preparations. The potency of dynorphin-(1-13) relative to that of ethylketocyclazocine (Mr 2266), a representative kappa-receptor agonist, in inhibiting the electrically evoked contractions of the guinea-pig ileum was found to be similar to that found with either mouse was deferens or rabbit ileum. Moreover, Mr 2266 was found to be several-fold more effective than naloxone to antagonize the agonist actions of both kappa-receptor agonists such as ethylketocyclazocine, ketocyclazocine and bremazocine, and dynorphin-(1-13) either in the guinea-pig ileum, mouse vas deferens, or in rabbit ileum. Additionally, dynorphin-(1-13) was found to have a significant inhibitory action on the rabbit vas deferens which had been shown to contain kappa-receptors exclusively. The data indicate that dynorphin-(1-13) acts as an endogenous agonist on kappa-receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cyclazocine / analogs & derivatives
  • Cyclazocine / pharmacology
  • Dynorphins*
  • Electric Stimulation
  • Endorphins / pharmacology*
  • Ethylketocyclazocine
  • Guinea Pigs
  • Ileum / drug effects
  • In Vitro Techniques
  • Male
  • Mice
  • Mice, Inbred ICR
  • Muscle Contraction / drug effects*
  • Muscle, Smooth / drug effects*
  • Naloxone / pharmacology
  • Peptide Fragments / pharmacology*
  • Rabbits
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / drug effects*
  • Receptors, Opioid, kappa
  • Vas Deferens / drug effects

Substances

  • Endorphins
  • Peptide Fragments
  • Receptors, Opioid
  • Receptors, Opioid, kappa
  • Naloxone
  • Ethylketocyclazocine
  • dynorphin (1-13)
  • Dynorphins
  • Cyclazocine