Muscarinic acetylcholine receptors as CNS drug targets

Pharmacol Ther. 2008 Feb;117(2):232-43. doi: 10.1016/j.pharmthera.2007.09.009. Epub 2007 Dec 20.

Abstract

Muscarinic acetylcholine receptors (mAChRs) are widely expressed in the CNS where they control a variety of neuronal functions. Due to their roles in a number of CNS processes, mAChRs have long been a target of the drug discovery industry; however, the only mAChR ligands approved for use in the clinic are non-selective antagonists for the treatment of Parkinson's disease. This article briefly reviews recent progress made in mAChR drug discovery for Alzheimer's disease (AD), schizophrenia and Parkinson's disease, with particular emphasis on novel target validation, as well as highlighting novel indications such as drug addiction.

Publication types

  • Review

MeSH terms

  • Alzheimer Disease / drug therapy
  • Alzheimer Disease / metabolism
  • Animals
  • Antiparkinson Agents / pharmacology
  • Antipsychotic Agents / pharmacology
  • Central Nervous System / drug effects*
  • Central Nervous System / metabolism
  • Central Nervous System Agents / pharmacology*
  • Central Nervous System Agents / therapeutic use
  • Humans
  • Muscarinic Agonists / pharmacology*
  • Muscarinic Agonists / therapeutic use
  • Muscarinic Antagonists / pharmacology*
  • Muscarinic Antagonists / therapeutic use
  • Parkinson Disease / drug therapy
  • Parkinson Disease / metabolism
  • Receptor, Muscarinic M1 / drug effects
  • Receptor, Muscarinic M1 / metabolism
  • Receptor, Muscarinic M2 / drug effects
  • Receptor, Muscarinic M2 / metabolism
  • Receptor, Muscarinic M4 / drug effects
  • Receptor, Muscarinic M4 / metabolism
  • Receptors, Muscarinic / drug effects*
  • Receptors, Muscarinic / metabolism
  • Schizophrenia / drug therapy
  • Schizophrenia / metabolism
  • Substance-Related Disorders / drug therapy
  • Substance-Related Disorders / metabolism

Substances

  • Antiparkinson Agents
  • Antipsychotic Agents
  • Central Nervous System Agents
  • Muscarinic Agonists
  • Muscarinic Antagonists
  • Receptor, Muscarinic M1
  • Receptor, Muscarinic M2
  • Receptor, Muscarinic M4
  • Receptors, Muscarinic