1. Francis Crick Institute, UK
2. University of Leicester, UK
3. University College London, UK
4. King's College London, UK
5. Monash University, Australia
6. PerkinElmer, UK
7. University of California Irvine, USA
8. Lilly Research Laboratories, USA
9. Nippon Boehringer Ingleheim, Japan
10. University of Mainz, Germany
11. University of Frankfurt, Germany
12. University of Melbourne, Australia
13. University of Washington, USA
14. Pfizer, USA
15. National Institutes of Health, USA

Abstract

Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [53]) 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 G_q/11 proteins, whilst M₂ and M₄ mAChRs predominantly couple to G_i/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. Of note, it has been observed that mAChRs dimerise reversibly [134] and that dimerisation/oligomerisation can be affected by ligands [183, 196].

Contents

GtoPdb is an expert-driven guide to pharmacological targets and the substances that act on them. GtoPdb is a reference work which is most usefully represented as an on-line database. As in any publication this work should be appropriately cited, and the papers it cites should also be recognized. This document provides a citation for the relevant parts of the database, and also provides a reference list for the research cited by those parts. For further details see [40].

Please note that the database version for the citations given in GtoPdb are to the most recent preceding version in which the family or its subfamilies and targets were substantially changed. The links below are to the current version. If you need to consult the cited version, rather than the most recent version, please contact the GtoPdb curators.

Database links

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