- cholinergic receptor, muscarinic 1, CNS
- Available assay modes
- Agonist, Inverse agonist, Antagonist, PAM, NAM
- à la carte, Mouse non-orphan GPCRs
Acetylcholine receptors (muscarinic)Muscarinic acetylcholine receptors (mAChRs) are activated by the endogenous agonist acetylcholine. All five (M1-M5) mAChRs are ubiquitously expressed in the human body and are therefore attractive targets for many disorders. Functionally, M1, M3, and M5 mAChRs preferentially couple to Gq/11 proteins, whilst M2 and M4 mAChRs predominantly couple to Gi/o proteins. Both agonists and antagonists of mAChRs are clinically approved drugs, including pilocarpine for the treatment of elevated intra-ocular pressure and glaucoma, and atropine for the treatment of bradycardia and poisoning by muscarinic agents such as organophosphates.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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