GtoPdb v.2023.1中乙酰胆碱受体(毒蕈碱)

IUPHAR/BPS Guide to Pharmacology CITE Pub Date : 2023-04-26 DOI:10.2218/gtopdb/f2/2023.1

Nigel J. M. Birdsall, Sophie Bradley, David A. Brown, Noel J. Buckley, R.A. John Challiss, Arthur Christopoulos, Richard M. Eglen, Frederick Ehlert, Christian C. Felder, Rudolf Hammer, Heinz J. Kilbinger, Günter Lambrecht, Chris Langmead, Fred Mitchelson, Ernst Mutschler, Neil M. Nathanson, Roy D. Schwarz, David Thal, Andrew B. Tobin, Celine Valant, Jurgen Wess

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引用次数: 0

摘要

毒蕈碱乙酰胆碱受体(mAChRs)(由NC-IUPHAR毒蕈碱乙酰胆碱受体小组委员会[53]商定的命名)被内源性激动剂乙酰胆碱激活。所有五种(M1-M5) machr在人体中普遍表达，因此是许多疾病的有吸引力的靶点。在功能上，M1、M3和M5 machr优先与Gq/11蛋白结合，而M2和M4 machr主要与Gi/o蛋白结合。machr的激动剂和拮抗剂都是临床批准的药物，包括用于治疗眼压升高和青光眼的匹罗卡品，以及用于治疗心动过缓和有机磷等毒蕈碱类药物中毒的阿托品。值得注意的是，已经观察到，machr二聚化是可逆的[134]，二聚化/寡聚化可以受到配体的影响[183,196]。

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Acetylcholine receptors (muscarinic) in GtoPdb v.2023.1

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 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. Of note, it has been observed that mAChRs dimerise reversibly [134] and that dimerisation/oligomerisation can be affected by ligands [183, 196].

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