Shiraki Y, Akima M, Nabata H, Ohba Y, Hoshino E, Sakai K
Jpn J Pharmacol. 1981 Dec;31(6):921-9. doi: 10.1254/jjp.31.921.
The hypotensive mechanisms of N-(2-hydroxyethyl) nicotinamide nitrate (SG-75, Nicorandil) were studied in anesthetized dogs. Intravenous injections of SG-75 (0.03-1 mg/kg) decreased systemic blood pressure (SBP) and increased peripheral (coronary, renal, mesenteric and femoral) blood flow (PBF) dose-dependently. The duration of the PBF increase, however, was much shorter than that of the SBP decrease. When peripheral vascular beds were perfused by means of a pump under a constant perfusion pressure near the SBP, the duration and magnitude of the SBP decrease and the PBF increase were equal. In doses of 0.03-0.3 mg/kg i.v., SG-75 did not significantly affect pulse pressure, heart rate, aortic blood flow, left ventricular pressure (LVP) and LVdP/dt max. Intra-arterial injections of SG-75 (0.003-1 mg) increased coronary, renal, mesenteric and femoral blood flow dose-dependently, without affecting SBP and cardiac function. In heart-lung preparations the drug (0.1-2 mg) did not cause cardiodepression. No hypotensive effect was observed following the administration of SG-75 (3 mg) into the cisterna magna. The results indicate that the hypotensive effect of SG-75 may be due mainly to its peripheral mechanisms, relating to vasodilation.
在麻醉犬中研究了硝酸N-(2-羟乙基)烟酰胺（SG-75，尼可地尔）的降压机制。静脉注射SG-75（0.03-1毫克/千克）可剂量依赖性地降低体循环血压（SBP）并增加外周（冠状动脉、肾、肠系膜和股动脉）血流量（PBF）。然而，PBF增加的持续时间比SBP降低的持续时间短得多。当通过泵在接近SBP的恒定灌注压力下灌注外周血管床时，SBP降低和PBF增加的持续时间和幅度相等。静脉注射剂量为0.03-0.3毫克/千克时，SG-75对脉压、心率、主动脉血流量、左心室压力（LVP）和LVdP/dt max无明显影响。动脉内注射SG-75（0.003-1毫克）可剂量依赖性地增加冠状动脉、肾、肠系膜和股动脉血流量，而不影响SBP和心脏功能。在心肺制备中，该药物（0.1-2毫克）不会引起心脏抑制。向小脑延髓池注射SG-75（3毫克）后未观察到降压作用。结果表明，SG-75的降压作用可能主要归因于其与血管舒张有关的外周机制。
