Muscarinic Acetylcholine Receptors


Muscarinic acetylcholine receptors play a key role in the regulation of signal transduction in the central and peripheral nervous systems.

Keywords: receptorG protein signal transduction

Figure 1.

Diagram of the heptahelical structure of a mAChR, interacting with a heterotrimeric G protein to regulate the activity of an effector protein. The glycosylated N‐terminal region of the mAChR is extracellular.



Anagnostaras S, Murphy GG, Hamilton SE et al. (2003) Selective cognitive dysfunction in acetylcholine M1 muscarinic receptor mutant mice. Nature Neurosciences 6: 51–58.

Felsch JS, Cachero TG and Peralta EG (1998) Activation of protein tyrosine kinase PYK2 by the m1 muscarinic acetylcholine receptor. Proceedings of the National Academy of Sciences of the USA 95: 5051–5056.

Habecker BA, Wang H and Nathanson NM (1993) Multiple second messenger pathways mediate agonist regulation of muscarinic receptor mRNA expression. Biochemistry 32: 4986–4990.

Liu C, Ding JM, Faiman LE and Gillette MU (1997) Coupling of muscarinic cholinergic receptors and cGMP in nocturnal regulation of the suprachiasmatic circadian clock. Journal of Neuroscience 17: 659–666.

Liu J, Blin N, Conklin BR and Wess J (1996) Molecular mechanisms involved in muscarinic acetylcholine receptor‐mediated G protein activation studied by insertion mutagenesis. Journal of Biological Chemistry 271: 6172–6178.

Liu J, Schoneberg T, van Rhee M and Wess J (1995) Mutational analysis of the relative orientation of transmembrane helices I and VII in G protein‐coupled receptors. Journal of Biological Chemistry 270: 19532–19539.

Pals‐Rylaarsdam R and Hosey MM (1997) Two homologous phosphorylation domains differentially contribute to desensitization and internalization of the m2 muscarinic acetylcholine receptor. Journal of Biological Chemistry 272: 14152–14158.

Spalding TA, Burstein ES, Wells JW and Brann MR (1997) Constitutive activation of the m5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6. Biochemistry 36: 10109–10116.

Thomas LS, Chmelar RS, Lu C, Halvorsen SW and Nathanson NM (1997) Tissue specific regulation of G‐protein coupled inwardly rectifying K+ channel expression by muscarinic receptor activation in ovo. Journal of Biological Chemistry 272: 29958–29962.

Tzavara ET, Bymaster FP, Felder CC et al. (2003) Dysregulated hippocampal acetylcholine neurotransmission and impaired cognition in M2, M4 and M2/M4 muscarinic receptor knockout mice. Molecular Psychiatry 8: 673–679.

Further Reading

Bourne HR (1997) How receptors talk to trimeric G proteins. Current Opinion in Cell Biology 9: 134–142.

Brown JH and Taylor P (1996) Muscarinic receptor agonists and antagonists. In: Gardman JG, Limbird LE, Molinoff PB, Ruddon RW and Gilman AG (eds) Goodman's and Gilman's The Pharmacological Basis of Therapeutics, pp. 141–160. New York: McGraw‐Hill.

Caulfield MP and Birdsall NJM (1998) International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors. Pharmacological Reviews 50: 279–290.

DiChiara G, Morelli M and Consolo S (1994) Modulatory functions of neurotransmitters in the striatum: ACh/dopamine/NMDA interactions. Trends in Neurosciences 17: 228–233.

Gutking JS (1998) The pathways connecting G protein‐coupled receptors to the nucleus through divergent mitogen‐activated protein kinase cascades. Journal of Biological Chemistry 273: 1839–1842.

Krupnick JG and Benovic JL (1998) The role of receptor kinases and arrestins in G protein‐coupled receptor regulation. Annual Review of Pharmacology and Toxicology 38: 289–319.

Levey AI (1996) Muscarinic acetylcholine receptor expression in memory circuits: implications for treatment of Alzheimer disease. Proceedings of the National Academy of Sciences of the USA 93: 13541–13546.

Nathanson NM (1989) Regulation and development of muscarinic acetylcholine number and function. In: Brown JH (ed.) The Muscarinic Receptors, pp. 419–454. Clifton, NJ: Humana Press.

Wess J (2003) Novel insights into muscarinic acetylcholine receptor function using gene targeting technology. Trends in Pharmacological Sciences 24: 414–420.

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How to Cite close
Nathanson, Neil M(Jan 2006) Muscarinic Acetylcholine Receptors. In: eLS. John Wiley & Sons Ltd, Chichester. [doi: 10.1038/npg.els.0004078]