Molecular mechanisms of regulation of neuronal muscarinic receptor sensitivity

Esam E. El-Fakahany, Catherine L. Cioffi

Research output: Contribution to journalArticlepeer-review

26 Scopus citations


Like other neurotransmitter receptors, muscarinic acetylcholine receptors are subject to regulation by the state of receptor activation. Prolonged increases in the concentration of muscarinic agonists result in a decrease in receptor density and loss of receptor sensitivity, both in vivo and in vitro. On the other hand, when the receptor is deprived of acetylcholine for a long duration in vivo, the receptor becomes more sensitive in responding to muscarinic agonists. However, it has been more difficult to demonstrate increases in receptor concentration that accompany this supersensitive state. The purpose of this review is to provide current information related to the characteristics of muscarinic receptor regulation and the molecular mechanisms underlying this phenomenon, regarding both the density of receptors and their transduction mechanisms. Furthermore, possible feedback regulatory roles of different second messenger signals are discussed. Particular emphasis is dedicated to molecular mechanisms of regulation of neuronal muscarinic receptors.

Original languageEnglish (US)
Pages (from-to)9-27
Number of pages19
JournalMolecular Membrane Biology
Issue number1
StatePublished - Jan 1 1990


  • Acetylcholine
  • Adenylate cyclase
  • Brain
  • Cyclic GMP
  • Desensitization
  • Down-regulation
  • Muscarinic receptor
  • Neurons
  • Phosphoinositide hydrolysis
  • Receptor subtypes
  • Second messengers
  • Supersensitivity
  • Up-regulation

Fingerprint Dive into the research topics of 'Molecular mechanisms of regulation of neuronal muscarinic receptor sensitivity'. Together they form a unique fingerprint.

Cite this