Activation of G protein by opioid receptors: role of receptor number and G-protein concentration

Eur J Pharmacol. 2000 May 19;396(2-3):67-75. doi: 10.1016/s0014-2999(00)00212-0.

Abstract

The collision-coupling model for receptor-G-protein interaction predicts that the rate of G-protein activation is dependent on receptor density, but not G-protein levels. C6 cells expressing mu- or delta-opioid receptors, or SH-SY5Y cells, were treated with beta-funaltrexamine (mu) or naltrindole-5'-isothiocyanate (delta) to decrease receptor number. The time course of full or partial agonist-stimulated ¿35SGTPgammaS binding did not vary in C6 cell membranes containing <1-25 pmol/mg mu-opioid receptor, or 1. 4-4.3 pmol/mg delta-opioid receptor, or in SHSY5Y cells containing 0. 16-0.39 pmol/mg receptor. The association of ¿35SGTPgammaS binding was faster in membranes from C6mu cells than from C6delta cells. A 10-fold reduction in functional G-protein, following pertussis toxin treatment, lowered the maximal level of ¿35SGTPgammaS binding but not the association rate. These data indicate a compartmentalization of opioid receptors and G protein at the cell membrane.

Publication types

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

MeSH terms

  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / pharmacology
  • GTP-Binding Proteins / analysis
  • GTP-Binding Proteins / physiology*
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Receptors, Opioid, delta / analysis
  • Receptors, Opioid, delta / physiology*
  • Receptors, Opioid, mu / analysis
  • Receptors, Opioid, mu / physiology*
  • Tumor Cells, Cultured

Substances

  • Receptors, Opioid, delta
  • Receptors, Opioid, mu
  • Enkephalin, Ala(2)-MePhe(4)-Gly(5)-
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • GTP-Binding Proteins