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Review
. 2019 Mar 20;10(3):1025-1034.
doi: 10.1021/acschemneuro.8b00481. Epub 2018 Oct 17.

The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation

Aaron M Bender  1   2 , Aaron T Garrison  1   2 , Craig W Lindsley  1   2
Affiliations
Review

The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation

Aaron M Bender et al. ACS Chem Neurosci. .

Abstract

The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) was the most recent mAChR to be cloned and has since emerged as a potential therapeutic target for a number of indications. Early studies with knockout animals have provided clues to the receptor's role in physiological processes related to Alzheimer's disease, schizophrenia, and addiction, and until recently, useful subtype-selective tools to further probe the pharmacology of M5 have remained elusive. Small-molecule allosteric modulators have since gained traction as a means by which to selectively examine muscarinic pharmacology. This review highlights the discovery and optimization of M5 positive allosteric modulators (PAMs) and negative allosteric modulators (NAMs).

Keywords: Alzheimer’s disease; M5; addiction; allosteric modulator; knockout; muscarinic; schizophrenia.

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