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RESEARCH PRODUCT

Acetylcholine receptors (muscarinic) (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database

Celine ValantFred MitchelsonNoel J. BuckleyDavid BrownNeil M. NathansonRoy D. SchwarzNigel J. M. BirdsallChristian C. FelderRudolf HammerChris LangmeadArthur ChristopoulosGünter LambrechtFrederick J. EhlertRichard M. EglenJürgen WessSophie J. BradleyErnst MutschlerHeinz KilbingerAndrew B. TobinR. A. John Challiss

subject

chemistry.chemical_compoundChemistryAllosteric regulationMuscarinic acetylcholine receptormedicineStrychnineMuscarinic acetylcholine receptor M1PharmacologyAcetylcholineEndogenous agonistmedicine.drugAcetylcholine receptorG protein-coupled receptor

description

Muscarinic acetylcholine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [45]) are GPCRs of the Class A, rhodopsin-like family where the endogenous agonist is acetylcholine. In addition to the agents listed in the table, AC-42, its structural analogues AC-260584 and 77-LH-28-1, N-desmethylclozapine, TBPB and LuAE51090 have been described as functionally selective agonists of the M1 receptor subtype via binding in a mode distinct from that utilized by non-selective agonists [243, 242, 253, 155, 154, 181, 137, 11, 230]. There are two pharmacologically characterised allosteric sites on muscarinic receptors, one defined by it binding gallamine, strychnine and brucine, and the other defined by the binding of KT 5720, WIN 62,577, WIN 51,708 and staurosporine [161, 162].

yearjournalcountryeditionlanguage
2019-09-16IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/f2/2019.4