Acetylcholine receptors (muscarinic) in GtoPdb v.2021.2

  • Nigel J. M. Birdsall Francis Crick Institute
  • Sophie Bradley University of Leicester https://orcid.org/0000-0002-0035-4090
  • David A. Brown University College London
  • Noel J. Buckley King's College London
  • R.A. John Challiss University of Leicester
  • Arthur Christopoulos Monash University https://orcid.org/0000-0003-4442-3294
  • Richard M. Eglen PerkinElmer
  • Frederick Ehlert University of California Irvine
  • Christian C. Felder Lilly Research Laboratories
  • Rudolf Hammer Nippon Boehringer Ingleheim
  • Heinz J. Kilbinger University of Mainz
  • Günter Lambrecht University of Frankfurt
  • Chris Langmead Monash University
  • Fred Mitchelson University of Melbourne
  • Ernst Mutschler University of Frankfurt
  • Neil M. Nathanson University of Washington
  • Roy D. Schwarz Pfizer
  • David Thal Monash University https://orcid.org/0000-0002-0325-2524
  • Andrew B. Tobin University of Leicester https://orcid.org/0000-0002-1807-3123
  • Celine Valant Monash University https://orcid.org/0000-0002-2509-7465
  • Jurgen Wess National Institutes of Health

Abstract


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

Published
25-Jun-2021
How to Cite
Birdsall, N. J. M., Bradley, S., Brown, D. A., Buckley, N. J., Challiss, R. J., Christopoulos, A., Eglen, R. M., Ehlert, F., Felder, C. C., Hammer, R., Kilbinger, H. J., Lambrecht, G., Langmead, C., Mitchelson, F., Mutschler, E., Nathanson, N. M., Schwarz, R. D., Thal, D., Tobin, A. B., Valant, C. and Wess, J. (2021) “Acetylcholine receptors (muscarinic) in GtoPdb v.2021.2”, IUPHAR/BPS Guide to Pharmacology CITE, 2021(2). doi: 10.2218/gtopdb/F2/2021.2.
Section
Summaries