Nicorandil (Synonyms: 2-Nicotinamidoethyl nitrate, SG-75) |
| カタログ番号GC15552 |
ニコランジル (SG-75) は強力なカリウム チャネル活性化因子であり、血管ヌクレオシド二リン酸依存性 K+ チャネルと心臓 ATP 感受性 K+ チャネル (KATP) を標的とします。
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Cas No.: 65141-46-0
Sample solution is provided at 25 µL, 10mM.
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Nicorandil (SG-75) is potassium channel activator.
Nicorandil (SG-75) 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[1][2].
References:
[1]. Nakae, I., et al., Effects of intravenous nicorandil on coronary circulation in humans: plasma concentration and action mechanism. J Cardiovasc Pharmacol, 2000. 35(6): p. 919-25.
[2]. Sauzeau, V., et al., Cyclic GMP-dependent protein kinase signaling pathway inhibits RhoA-induced Ca2+ sensitization of contraction in vascular smooth muscle. J Biol Chem, 2000. 275(28): p. 21722-9.
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