Acetylcholine receptor: covalent attachment of depolarizing groups at the active site

Science. 1969 Jun 20;164(3886):1420-1. doi: 10.1126/science.164.3886.1420.

Abstract

Following reduction of the acetylcholine receptor in the electroplax with dithiothreitol, the quaternary ammonium compounds bromoacetylcholine bromide and the p-nitrophenyl ester of (p-carboxyphenyl) trimethylammonium iodide react near the active site probably with a sulfhydryl group. The covalently attached quaternary ammonium moieties additionally interact with the active site noncovalently to activate the receptor and cause depolarization of the cell.

MeSH terms

  • Acetylcholine*
  • Animals
  • Binding Sites*
  • Bromides / pharmacology
  • Eels
  • Iodides / pharmacology
  • Quaternary Ammonium Compounds / pharmacology
  • Receptors, Drug*
  • Sulfhydryl Compounds / pharmacology

Substances

  • Bromides
  • Iodides
  • Quaternary Ammonium Compounds
  • Receptors, Drug
  • Sulfhydryl Compounds
  • Acetylcholine