达非那新

Darifenacin(UK88525)是M3毒蕈碱型受体拮抗剂,pKi为8.9。

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

信号通路 >> 神经信号通路 >> mAChR

研究领域 >> 神经疾病

[1]. Hegde SS, et al. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol, 1997, 120(8), 1409-1418.

[2]. Miller DW, et al. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn, 2011, 30(8), 1633-1638.

[3]. Iijima K, et al. Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. Eur Urol, 2007, 52(3), 842-847.

[4]. Lu XZ, et al. Activation of M3 cholinoceptors attenuates vascular injury after ischaemia/reperfusion by inhibiting the Ca2+/calmodulin-dependent protein kinase II pathway. Br J Pharmacol. 2015 Dec;172(23):5619-33.

[5]. Yu H, et al.Acetylcholine acts through M3 muscarinic receptor to activate the EGFR signaling and promotes gastric cancer cell proliferation. Sci Rep. 2017 Jan 19;7:40802.

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