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Updated: Feb 4, 2026

Subcutaneous Administration of Muscarinic Antagonists and Triple-Immunostaining of the Levator Auris Longus Muscle in Mice
Published on: September 8, 2011
The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation
Aaron M Bender1,2, Aaron T Garrison1,2, Craig W Lindsley1,2
1Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University Medical Center , Nashville , Tennessee 37232 , United States.
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).
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