Interactions of d-tubocurarine with the nicotinic acetylcholine receptor/channel molecule

J Pharmacol Exp Ther. 1982 Jan;220(1):172-7.

Abstract

The interactions of d-tubocurarine (d-TC) with the ionic channel of the nicotinic acetylcholine receptor were studied by biochemical methods in Torpedo electric organ membranes and by electrophysiological methods on frog sciatic nerve-sartorius muscle preparation. Torpedo membranes were treated with alpha-bungarotoxin to inhibit the acetylcholine receptor sites, then binding of [3H]perhydrohistrionicotoxin to the ionic channel sites was studied and found to be inhibited by d-TC. At 37 degrees C, the Ki of d-TC was 10 microM, and at 22 degrees C it was 100 microM. The affinity of d-TC for the ionic channel sites relative to that of perhydrohistrionicotoxin was constant at temperatures from 2-20 degrees C, but increased at higher temperatures up to 37 degrees C. The peak endplate current amplitude was depressed with 1 to 2 microM d-TC in a voltage-dependent manner, with considerable departure from linearity at 10 and 30 degrees C. The effect of d-TC on spontaneous miniature endplate currents was similar and slightly more potent. The time constant of endplate current decay was decreased by d-TC (1 and 2 microM) at temperatures of 10, 15 and 30 degrees C. The channel lifetime was reduced by d-TC, but channel conductance was unaffected. It is suggested that d-TC interacts with both the acetylcholine receptor sites as well as its ionic channel sites in closed and open conformations.

Publication types

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

MeSH terms

  • Amphibian Venoms / metabolism
  • Animals
  • Binding, Competitive
  • Bungarotoxins / pharmacology
  • Electrophysiology
  • In Vitro Techniques
  • Ion Channels / drug effects*
  • Kinetics
  • Motor Endplate / drug effects
  • Rana pipiens
  • Receptors, Cholinergic / drug effects*
  • Receptors, Nicotinic / drug effects*
  • Receptors, Nicotinic / metabolism
  • Torpedo
  • Tubocurarine / metabolism
  • Tubocurarine / pharmacology*

Substances

  • Amphibian Venoms
  • Bungarotoxins
  • Ion Channels
  • Receptors, Cholinergic
  • Receptors, Nicotinic
  • perhydrohistrionicotoxin
  • Tubocurarine