Muscarinics

Muscarinic acetylcholine receptors (mAChRs) are a critical subfamily of G-protein coupled receptors (GPCRs) found in the central nervous system and periphery which mediate acetylcholine signaling and thus modulate a wide range of physiological processes. These receptors have therefore been long sought out as targets to potentiate acetylcholine signaling within different regions of the body. Action at these receptors has been observed for over one hundred years, and as a result of this history and humanity's ever-increasing understanding of the structure and function of mAChRs, multiple drugs targeting these receptors have been approved to date, treating conditions ranging from chronic obstructive pulmonary disease (COPD) to xerostomia, with a multitude of additional candidates currently in clinical trials or the drug development pipeline. The present chapter will provide a brief account of the history, structure, and function of these receptors as well as an overarching view of drug development within this field to date.

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