Opioids increase potassium conductance in submucous neurones of guinea-pig caecum by activating delta-receptors

Br J Pharmacol. 1986 Jun;88(2):315-22. doi: 10.1111/j.1476-5381.1986.tb10207.x.

Abstract

Intracellular records were made from neurones in the submucous plexus of the guinea-pig caecum. [Met5]enkephalin, [Leu5]enkephalin, [D-Ala2,D-Leu5]enkephalin (DADLE) and [D-Ser2,Leu5]enkephalin-Thr (DSLET) hyperpolarized the membrane when applied in concentrations of 30 nm-10 microM. Normorphine, [D-Ala2, MePhe4,Gly5]enkephalin-ol (DAGO), [D-Ala2,MePhe4,Met(0)5]enkephalin-ol (FK33824), dynorphin A and tifluadom had no effect at concentrations up to 10 microM. The hyperpolarization resulted from an increase in the membrane potassium conductance. Hyperpolarizations induced by [Met5]enkephalin were antagonized competitively by naloxone and by N-bisallyl[aminoisobutyrate2,3, Leu5]enkephalin (ICI 174864). The Schild plots for these antagonisms had slopes not different from one, and the dissociation equilibrium constants among individual neurones were 5-50 nM for naloxone and 5-60 nM for ICI 174864. The results indicate that the opioid receptors on guinea-pig submucous neurones which are coupled to potassium channels are of the delta-type.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adrenergic alpha-Agonists / pharmacology
  • Animals
  • Cecum / drug effects
  • Cecum / physiology
  • Endorphins / pharmacology*
  • Enkephalin, Leucine / pharmacology
  • Enkephalin, Methionine / pharmacology
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Membrane Potentials / drug effects
  • Muscle, Smooth / physiology*
  • Neural Conduction / drug effects
  • Neurons / physiology*
  • Norepinephrine / pharmacology
  • Potassium / physiology*
  • Receptors, Opioid / physiology*
  • Receptors, Opioid, delta
  • Somatostatin / pharmacology

Substances

  • Adrenergic alpha-Agonists
  • Endorphins
  • Receptors, Opioid
  • Receptors, Opioid, delta
  • Somatostatin
  • Enkephalin, Methionine
  • Enkephalin, Leucine
  • Potassium
  • Norepinephrine