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Pharmacol Ther. 2003 May;98(2):197-220.

Regulation of muscarinic acetylcholine receptor signaling.

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  • 1Institut f├╝r Pharmakologie, Universit├Ątsklinikum Essen, Hufelandstrasse 55, D-45122, Essen, Germany.


Multiple mechanisms regulate the signaling of the five members of the family of the guanine nucleotide binding protein (G protein)-coupled muscarinic acetylcholine (ACh) receptors (mAChRs). Following activation by classical or allosteric agonists, mAChRs can be phosphorylated by a variety of receptor kinases and second messenger-regulated kinases. The phosphorylated mAChR subtypes can interact with beta-arrestin and presumably other adaptor proteins as well. As a result, the various mAChR signaling pathways may be differentially altered, leading to short-term or long-term desensitization of a particular signaling pathway, receptor-mediated activation of the mitogen-activated protein kinase pathway downstream of mAChR phosphorylation, as well as long-term potentiation of mAChR-mediated phospholipase C stimulation. Agonist activation of mAChRs may also induce receptor internalization and down-regulation, which proceed in a highly regulated manner, depending on receptor subtype and cell type. In this review, our current understanding of the complex regulatory processes that underlie signaling of mAChR is summarized.

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