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Tolbutamide

甲苯磺丁脲

Mechanism of action:

Tolbutamide 是一種磺醯脲類(sulfonylurea)衍生物。Tolbutamide 能結合並抑制胰島 β 細胞膜上的磺醯脲受體 1(SUR1),此受體為 ATP-敏感鉀離子通道蛋白(ATP-sensitive potassium channel)的調節亞基。被 tolbutamide 抑制後,鉀離子外流減少,細胞膜發生去極化(depolarization)。去極化會造成鈣離子通道(calcium channel)開啟,鈣離子內流增加,促使胰島素釋放。

​Reference(s):

Zhou SF et al. (2009). Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem.

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