| Description | Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain. |
| In vitro | Nicorandil （100 mM）能增加黄素蛋白氧化，但不能增加膜电流。Nicorandil 浓度高出 10 倍时，线粒体 K（ATP）和表面 K（ATP）通道都会被吸引。Nicorandil 能降低缺血造粒模型中的细胞死亡率，然而线粒体 K（ATP）通道阻断剂 5-hydroxydecanoate 能阻止这种心脏保护作用。[1] Nicorandil （100 mM）可抑制 TUNEL 阳性、细胞色素 c 转位、caspase-3 激活和线粒体内膜电位（Delta(Psi)(m)）耗散。荧光激活细胞分拣机对用荧光 Delta(Psi)(m) 指示剂四甲基罗丹明乙酯（TMRE）染色的细胞进行分析表明，Nicorandil 以浓度依赖性方式防止 Delta(Psi)(m) 去极化（EC(50) 约为 40 mM，到 100 mM时达到饱和）。[2]Nicorandil 在两种转染细胞中都能激活一个弱内向整流、对格列本脲敏感的 80 pS K+ 通道。Nicorandil 能优先激活含有 SUR2B 的 K（ATP）通道D HEK293T 细胞。[3] Nicorandil （100 mM）能明显抑制 20 mM Water2 诱导的细胞核 TUNEL 阳性的细胞数量和 Caspase-3 活性的增加。Nicorandil 能以浓度依赖性方式防止 Water2 诱导的 DeltaPsim 损失。[4] |
| Synonyms | SG-75, 尼可地尔 |
| molecular weight | 211.17 |
| Molecular formula | C8H9N3O4 |
| CAS | 65141-46-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 80.5 mM DMSO: 50 mg/mL (236.76 mM) |
| References | 1. Sato T, et al. J Am Coll Cardiol, 2000, 35(2), 514-518. 2. Akao M, et al. J Am Coll Cardiol, 2002, 40(4), 803-810. 3. Szczepanik AM, et al. J Pharmacol Exp Ther, 1996, 278(2), 913-920. 4. Teshima Y, et al. Brain Res, 2003, 1990(1-2), 45-50. 5. Sathish V, et al. Mol Cell Biochem, 2003, 243(1-2), 133-138. |