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背景说明:Gap19 是一种衍生自 Cx43 细胞质环 (CL) 九个氨基酸的肽,一种有效的,选择性连接蛋白 43 (Cx43) 半通道阻滞剂。Gap19 可以防止 C 末端 (CT) 与 CL 的分子内相互作用。Gap19 不阻断 GJ 通道或 Cx40/pannexin-1 半通道。Gap19 对心肌具有保护作用。 In Vivo:Gap19 (iv; 25 mg/kg; 10 min before ligation) significantly reduces the infarct size by approximately one-fifth. In Vitro:Gap19 (250 μM; for 30 min ) decreases mitochondrial potassium uptake. Gap19 (400 μM) inhibits unitary hemichannel currents in HeLa-Cx43 cells. Gap19 (100 μM) inhibits hemichannel unitary currents in ventricular cardiomyocytes. Gap19 (250 μM, 30 min) protects against myocardial ischemia/reperfusion injury in vitro and in vivo. 参考文献:[1]. Boengler K, et al. Connexin 43 impacts on mitochondrial potassium uptake. Front Pharmacol. 2013 Jun 6;4:73. [2]. Wang N, et al. Selective inhibition of Cx43 hemichannels by Gap19 and its impact on myocardial ischemia/reperfusion injury. Basic Res Cardiol. 2013 Jan;108(1):309.
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