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

  • Nigel J. M. Birdsall Francis Crick Institute
  • Sophie Bradley University of Leicester
  • David A. Brown University College London
  • Noel J. Buckley King's College London
  • R.A. John Challiss University of Leicester
  • Arthur Christopoulos Monash University
  • 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
  • Andrew B. Tobin University of Leicester
  • Celine Valant Monash University
  • Jurgen Wess National Institutes of Health


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].
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., Tobin, A. B., Valant, C. and Wess, J. (2019) “Acetylcholine receptors (muscarinic) (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database”, IUPHAR/BPS Guide to Pharmacology CITE, 2019(4). doi: 10.2218/gtopdb/F2/2019.4.