神经系统疾病治疗靶点——毒蕈碱乙酰胆碱受体 - 知乎
M1、M3和M5受体亚型是兴奋性的，并与Gq/G11偶联，负责激活磷脂酶C-β (PLC-β)，导致信号分子肌醇三磷酸 (IP3)和二酰基甘油 (DAG)的产生，而M2和M4受体亚型是抑制性的，并与Gi/Go偶联，导致腺苷酸环化酶的抑制和cAMP的减少, M2也被证明与Gs和Gq蛋白弱偶联 [7,8]（图2）。
乙酰胆碱对胃肠道运动的调控机制 - 知乎
2023年11月21日 · 乙酰胆碱是通过毒蕈碱受体（mAChR）来调控胃肠道平滑肌的收缩的，其中毒蕈碱受体主要是 M2 受体（M2R）和 M3 受体（M3R）。 在2021年发表在 IJMS 中的一篇综述中，作者通过敲除特定受体的小鼠对胆碱能递质的响应，…
Muscarinic Acetylcholine Receptor M3 - ScienceDirect
The M3 muscarinic acetylcholine receptor (M3R) belongs to the superfamily of G protein-coupled receptors and, following ligand dependent activation, selectively activates G proteins of the Gq/11 family. From: Trends in Endocrinology & Metabolism, 2011
Two-step structural changes in M3 muscarinic receptor ... - Nature
2023年3月8日 · Our results reveal that the G protein activation evokes a two-step change in the hM3R structure, including the fast step mediated by G q protein binding and the subsequent slower step mediated by...
Structure-guided development of selective M3 muscarinic ... - PNAS
Starting from a single amino acid difference in the orthosteric pockets in M2 muscarinic acetylcholine receptor (M2R) and M3R, we developed an M3R-selective antagonist using molecular docking and structure-based design. The resulting M3R antagonist showed up to 100-fold selectivity over the M2R in affinity and 1,000-fold selectivity in vivo.
Structure and dynamics of the M3 muscarinic acetylcholine receptor
2012年2月22日 · We describe here the structure of the G q/11 -coupled M3 mAChR (‘M3 receptor’, from rat) bound to the bronchodilator drug tiotropium and identify the binding mode for this clinically important...
The role of M3-muscarinic receptor signaling in insulin secretion
2011年7月1日 · As a prototypical G q/11 -coupled receptor, activation of M3R induces the hydrolysis of membrane phospholipid phosphatidylinositol-4,5-biphosphate (PIP 2), catalyzed by phospholipase C (PLC). This generates two second messengers, inositol-1,4,5-trisphosphate (IP 3) and diacylglycerol (DAG).
毒覃碱型受体_百度百科
近年发现M 受体有五种亚型，M1受体主要分布于交感节后神经和胃壁细胞，受体激动引起兴奋和胃酸分泌；M2受体主要分布于心肌、平滑肌，激动引起心脏收缩力和心率降低；M3受体主要分布于腺体和血管平滑肌，引起平滑肌松弛和腺体分泌。 M4 和M5尚未找到与之相对应的药理学分型 。 M1、M2、M3这三种受体均有各自的选择性激动剂和拮抗剂，阿托品对这三种M受体均可阻断。 [1] 当 乙酰胆碱 与这类 受体 结合后，可产生一系列 副交感神经 末梢兴奋地效应，包括心脏活 …
The M3 Muscarinic Acetylcholine Receptor Can Signal through …
The M3 muscarinic acetylcholine receptor (M3R) is a G protein–coupled receptor (GPCR) that regulates important physiologic processes, including vascular tone, bronchoconstriction, and insulin secretion. It is expressed on a wide variety of cell ...
Muscarinic acetylcholine M receptors (mAChRs) belong to the G protein-coupled receptor (GPCR) superfamily and play a crucial role in regulating and controlling the release of acetylcholine (ACh). This review aims to focus on M3 receptor (M3R) subtype distribution, function, eficacy, …