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Nicorandil

CAS No. : 65141-46-0

MCE 国际站：Nicorandil

产品活性：Nicorandil (SG-75) 是有效的钾通道 (potassium channel) 激活剂，靶向血管核苷二磷酸依赖性 K⁺ 通道和心脏 ATP 敏感 K⁺ 通道 (K_ATP)。Nicorandil 是一种烟酰胺酯，具有血管舒张和心脏保护作用，并具有用于心绞痛和缺血性心脏病的潜力。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: Nicorandil (SG-75) activates ATP-sensitive K⁺ channels composed of Kir6.2 and either sulfonylurea receptor (SUR) 2A or 2B.
Nicorandil is a vasodilatory drug used to treat angina. Nicorandil (SG-75) stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). cGMP activates protein kinase G (PKG) which phosphorylates and inhibits GTPase RhoA and decreases Rho-kinase activity. Reduced Rho-kinase activity permits an increase in myosin phosphatase activity, decreasing the calcium sensitivity of the smooth muscle. PKG also activates the sarcolemma calcium pump to remove activating calcium. PKG acts on K+ channels to promote K+ efflux and the ensuing hyperpolarization inhibits voltage-gated calcium channels. Overall, this leads to relaxation of the smooth muscle and coronary vasodilation.

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