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Nicorandil

尼可地爾
Mechanism of action:
Nicorandil 同時具有一氧化氮血管擴張作用與增加鉀離子通道活性(potassium channel opener)的雙重機制。Nicorandil 的分子一端具有硝酸酯結構,能在血管平滑肌中釋放一氧化氮,活化鳥苷酸環化酶(guanylyl cyclase),增加 cGMP,使平滑肌放鬆,血管擴張。Nicorandil 的另一端能開啟 ATP-敏感性鉀離子通道(ATP-sensitive potassium channel),使鉀離子外流,引起細胞膜超極化(hyperpolarization),鈣離子通道關閉,鈣離子進入減少,血管平滑肌放鬆。
Reference(s):
1. Kukovetz WR et al. (1992). Molecular mechanism of action of nicorandil. J Cardiovasc Pharmacol.
2. Russ U et al. (2003). Binding and effect of K ATP channel openers in the absence of Mg²⁺. Br J Pharmacol.
3. Yamada M et al. (2004). The nucleotide-binding domains of sulfonylurea receptor 2A and 2B play different functional roles in nicorandil-induced activation of ATP-sensitive K+ channels. Mol Pharmacol.
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