Muscarinic acetylcholine receptors mAChRs

The mAChR receptor is a 7TM/G protein-coupled receptor (GPCR) family with five members (M1-M5). Muscarinic Ml and M3 receptor (mAChR) activation can stimulate the a-secretory pathway for processing of APP to yield greater amounts of sAPPa and, theoretically, less Ab peptide.36 M2 receptor activation may also inhibit sAPPa secretion. Ml agonists also decrease the tau protein phosphorylation and hyperphosphorylation resulting from ApoE deficiency and improve learning and memory in animal models with cholinergic deficits. Muscarinic agonists advanced to the clinic that include civemeline 11, alvameline 12, and xanomeline 13 have failed due to a lack of receptor selectivity, poor bioavailability, a lack of robust efficacy, and/or a narrow therapeutic index, usually gastrointestinal side effects.

Civemiline (11) Alvameline (12) Xanomeline (13)

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