Three allosteric modulators act at a common site, distinct from that of competitive antagonists, at muscarinic acetylcholine M2 receptors

J Pharmacol Exp Ther. 1997 Jul;282(1):278-85.

Abstract

Functional studies were conducted on guinea pig atrial muscarinic acetylcholine M2 receptors with the allosteric modulators heptane-1,7-bis(dimethyl-3'-phthalimidopropyl)ammonium bromide (C7/3'-phth), gallamine and alcuronium to determine whether these ligands are able to recognize a common accessory site. The three modulators inhibited the negative inotropic response to carbachol in this tissue. When used in combination, C7/3'-phth and gallamine or C7/3'-phth and alcuronium gave dose ratios that were either additive or underadditive. In contrast, the combinations of C7/3'-phth or alcuronium with the competitive antagonists, N-methylscopolamine or atropine, yielded supra-additive dose ratios. The data could be reconciled with a model involving a ternary complex between (1) the receptor, (2) carbachol, N-methylscopolamine or atropine acting at the orthosteric binding site and (3) C7/3'-phth, alcuronium or gallamine acting at a common, allosteric site with varying degrees of heterotropic cooperativity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alcuronium / pharmacology
  • Allosteric Regulation
  • Animals
  • Atropine / pharmacology
  • Female
  • Gallamine Triethiodide / pharmacology
  • Guinea Pigs
  • Male
  • Muscarinic Antagonists / pharmacology*
  • N-Methylscopolamine
  • Receptor, Muscarinic M2
  • Receptors, Muscarinic / drug effects*
  • Scopolamine Derivatives / pharmacology

Substances

  • Muscarinic Antagonists
  • Receptor, Muscarinic M2
  • Receptors, Muscarinic
  • Scopolamine Derivatives
  • Atropine
  • Gallamine Triethiodide
  • Alcuronium
  • N-Methylscopolamine