Open AccessAcetylcholine receptors (muscarinic) in GtoPdb v.2021.2
Author(s) -
N. J. M. Birdsall,
Sophie J. Bradley,
David A. Brown,
Noel J. Buckley,
R. A. J. Challiss,
Arthur Christopoulos,
Richard M. Eglen,
Frederick J. Ehlert,
Christian C. Felder,
Rudolf Hammer,
H. Kilbinger,
Günter Lambrecht,
Christopher J. Langmead,
F. Mitchelson,
E. Mutschler,
Neil M. Nathanson,
Roy D. Schwarz,
David M. Thal,
Andrew B. Tobin,
Céline Valant,
Jürgen Wess
Publication year - 2021
Publication title -
iuphar/bps guide to pharmacology cite
Language(s) - English
Resource type - Journals
ISSN - 2633-1020
DOI - 10.2218/gtopdb/f2/2021.2
Subject(s) - muscarinic acetylcholine receptor , pilocarpine , atropine , acetylcholine , muscarinic acetylcholine receptor m4 , muscarinic acetylcholine receptor m1 , muscarinic acetylcholine receptor m2 , muscarinic acetylcholine receptor m3 , muscarinic acetylcholine receptor m5 , pharmacology , chemistry , acetylcholine receptor , receptor , agonist , medicine , neuroscience , biology , epilepsy
Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [50]) 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.I