Wada S, Isono C, Ogawa K
Arzneimittelforschung. 1981;31(10):1685-7.
The effect of N-(2-hydroxyethyl)-nicotinamide nitrate ester (nicorandil) on rat heart monoamine oxidase (MAO) was investigated in vitro. MAO activity was assayed by the isotopic method with 14C-tryptamine as substrate. Nicorandil significantly inhibited MAO activity of rat heart mitochondria. The effect of nicorandil on the enzymatic kinetics of MAO of rat heart mitochondria indicates that the anti-anginal drug acts as a competitive inhibitor of MAO. The inhibitor constant (Ki) of nicorandil was 4.93 mmol/l. The Ki of nicorandil was fitted to the formula derived from the relationship between the Ki values of glyceryl trinitrate, erythrytol tetranitrate, mannitol hexanitrate and isosorbide dinitrate and the dose of these drugs recommended to relieve anginal pain in patients. The dose of nicorandil was 0.071 mmol (15.0 mg at a time). This value agreed with the clinical dose for patients (10--20 mg at a time).
在体外研究了N-(2-羟乙基)-烟酰胺硝酸酯（尼可地尔）对大鼠心脏单胺氧化酶（MAO）的作用。以14C-色胺为底物，采用同位素法测定MAO活性。尼可地尔显著抑制大鼠心脏线粒体的MAO活性。尼可地尔对大鼠心脏线粒体MAO酶动力学的影响表明，该抗心绞痛药物作为MAO的竞争性抑制剂起作用。尼可地尔的抑制常数（Ki）为4.93 mmol/l。尼可地尔的Ki符合由硝酸甘油、四硝酸赤藓醇、六硝酸甘露醇和二硝酸异山梨酯的Ki值与推荐用于缓解患者心绞痛疼痛的这些药物剂量之间的关系推导得出的公式。尼可地尔的剂量为0.071 mmol（一次15.0 mg）。该值与患者的临床剂量（一次10 - 20 mg）一致。
