Acetylcholine receptors (muscarinic)

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Muscarinic acetylcholine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [13]) 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 [6,46,52-53,64,78,82-83,86]. 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 [57-58].

Receptors

M1 receptor Show summary » More detailed page

M2 receptor Show summary » More detailed page

M3 receptor Show summary » More detailed page

M4 receptor Show summary » More detailed page

M5 receptor Show summary » More detailed page

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Arthur Christopoulos, Nigel J. M. Birdsall, David A. Brown, Noel J. Buckley, R.A. John Challiss, Richard M. Eglen, Frederick Ehlert, Christian C. Felder, Rudolf Hammer, Heinz J. Kilbinger, Günter Lambrecht, Chris Langmead, Fred Mitchelson, Ernst Mutschler, Neil M. Nathanson, Andrew B. Tobin, Jurgen Wess, Roy D. Schwarz. Acetylcholine receptors (muscarinic). Accessed on 04/09/2015. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=2.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.