Conversion of dynorphin-(1-9) to [Leu5]enkephalin by the mouse vas deferens in vitro

Eur J Pharmacol. 1985 Oct 8;116(1-2):159-63. doi: 10.1016/0014-2999(85)90197-9.

Abstract

The inhibitory action of dynorphin-(1-9) on the electrically stimulated mouse vas deferens was seen to be antagonised by the delta-selective opioid antagonist ICI 174864. The observed delta-receptor mediated responses were partially, but not totally, prevented by peptidase inhibitors which protect the C- and N-termini of dynorphin-(1-9). [3H]Dynorphin-(1-9) is rapidly degraded by slices of vasa deferentia of the mouse. The major product of this metabolism co-elutes with [Leu5]enkephalin on reverse phase HPLC. It is concluded that a major component of the inhibitory effects of dynorphin-(1-9) on the mouse vas deferens is mediated by degradation to [Leu5]enkephalin which in turn acts through delta-receptors. It is possible that in other in vitro and in vivo systems, the effects produced by dynorphin-(1-9) might be similarly mediated by delta-receptor activation.

MeSH terms

  • Animals
  • Benzomorphans / pharmacology
  • Chromatography, High Pressure Liquid
  • Dynorphins / metabolism*
  • Enkephalin, Leucine / analogs & derivatives
  • Enkephalin, Leucine / metabolism*
  • Enkephalin, Leucine / pharmacology
  • In Vitro Techniques
  • Male
  • Mice
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / metabolism*
  • Narcotic Antagonists / pharmacology
  • Peptide Fragments / metabolism*
  • Vas Deferens / metabolism

Substances

  • Benzomorphans
  • Narcotic Antagonists
  • Peptide Fragments
  • MR 2266
  • Enkephalin, Leucine
  • Dynorphins
  • dynorphin A (1-9)
  • N,N-diallyl-tyrosyl-alpha-aminoisobutyric acid-phenylalanyl-leucine