Effects of extracellular acetylcholine on muscarinic receptor binding assessed by [125I]dexetimide and a simple probe

Patricia M. Sánchez-Roa, Henry N. Wagner, Victor L. Villemagne, Edythe D. London, John R. Lever

Research output: Contribution to journalArticle

Abstract

New pharmacologic approaches to enhance brain cholinergic function focus on increasing intrasynaptic acetylcholine. We examined the usefulness of a simple probe and [125I]dexetimide to evaluate in vivo the effects of extracellular acetylcholine on muscarinic receptor binding in the mouse brain. After radiotracer injection continuous time/activity curves were generated over 330 min. [125I]Dexetimide reached a plateau at 90 min post-injection. To increase extracellular acetylcholine, the anticholinesterase physostigmine was administered at 120 min, producing a reversible decrease in [125I]dexetimide specific binding (23%) for 30 min. These findings demonstrate that dynamic changes in extracellular acetylcholine can be evaluated by displacement of [125I]dexetimide binding in vivo using a simple probe system. Copyright (C) 1998 Elsevier Science B.V.

Original languageEnglish (US)
Pages (from-to)207-211
Number of pages5
JournalEuropean Journal of Pharmacology
Volume358
Issue number3
DOIs
StatePublished - Oct 9 1998
Externally publishedYes

Keywords

  • Acetylcholine
  • Brain
  • Dexetimide
  • Muscarinic receptor
  • Physostigmine
  • Radiation detection system

ASJC Scopus subject areas

  • Pharmacology

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