Novel persistent activation of muscarinic M1 receptors by xanomeline

Eur J Pharmacol. 1997 Sep 3;334(1):R3-4. doi: 10.1016/s0014-2999(97)01162-x.

Abstract

The muscarinic agonists, xanomeline and carbachol, displayed similar intrinsic activities in stimulating neuronal nitric oxide synthase at muscarinic M1 receptors in Chinese hamster ovary (CHO) cells, with xanomeline being more potent. Pre-incubation (1 h) with 1 microM xanomeline, followed by extensive washing, resulted in a significantly elevated basal response, which was absent on co-incubation with atropine. This phenomenon was not observed with carbachol. This is the first report of a persistent, receptor-activating effect of a muscarinic agonist.

Publication types

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

MeSH terms

  • Animals
  • CHO Cells / drug effects
  • Carbachol / pharmacology*
  • Cricetinae
  • Enzyme Activation
  • Muscarinic Agonists / pharmacology*
  • Nitric Oxide Synthase / drug effects*
  • Nitric Oxide Synthase / metabolism
  • Pyridines / pharmacology*
  • Receptor, Muscarinic M1
  • Receptors, Muscarinic / drug effects*
  • Receptors, Muscarinic / metabolism
  • Thiadiazoles / pharmacology*
  • Transfection

Substances

  • Muscarinic Agonists
  • Pyridines
  • Receptor, Muscarinic M1
  • Receptors, Muscarinic
  • Thiadiazoles
  • Carbachol
  • xanomeline
  • Nitric Oxide Synthase