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文献和实验Overview of Receptor Allosterism
Figure 1.21.1 Allosterism between a receptor and its G protein: the effects of GTP on the competition between [3 H] N ‐methylscopolamine and the agonist, carbachol, at the muscarinic acetylcholine M2 receptor in rat myocardial membranes. Competition
of N‐benzyl brucine on the specific binding of [3 H]N‐methylscopolamine ([3 H]NMS (0.4 nM at the M2 receptor and 0.2 nM at the M3 receptor) in the absence or presence of unlabeled acetylcholine (ACh; 2 µM at the M2 receptor and 20 µM at the M3 receptor
DREADDs受体作用原理(Scott M. Sternson & Bryan L. Roth, Annu. Rev. Neurosci., 2014)2. 常见的DREADDs受体(1)Gq-DREADD和hM3Dq:最初的Gq-DREADD即hM3Dq,改造自人毒蕈碱型乙酰胆碱受体(the human muscarinic acetylcholine receptor,mAchRs)亚型M3(也称为hM3)。在正常生理状况下,hM3和乙酰胆碱结合,然后和Gq类G蛋白耦合受体耦合,作用于磷脂酶C、肌醇三磷酸
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