Sakai K, Ohba Y, Akima M, Kamiyama H, Hinohara Y, Nakano H
Jpn J Pharmacol. 1980 Dec;30(6):881-90. doi: 10.1254/jjp.30.881.
Pharmacodynamics and metabolism of N-(2-hydroxyethyl) nicotinamide nitrate (SG-75) were investigated in rats in relation to its main metabolic product. When SG-75 was orally administered, SG-75 and SG-86, a denitrate compound of SG-75, appeared in the blood. Within 7 yr, approximately 60% of the administered SG-75 were recovered in the urine as SG-86. When administered intraduodenally, SG-75 was rapidly absorbed and transferred in an unaltered form into the portal vein. SG-75 possessed hypotensive and coronary vasodilating actions, while SG-86 had little effect on the cardiovascular system. The coronary vasodilating effects of SG-75 k(0.3-20 micrograms i.a.) were unaffected by the continuous infusion of SG-86 into the coronary perfusion system, even in large doses (50 micrograms/min, or 500 micrograms/min).
研究了硝酸N-(2-羟乙基)烟酰胺（SG-75）在大鼠体内的药效学和代谢及其主要代谢产物。口服SG-75后，SG-75及其脱硝酸盐化合物SG-86出现在血液中。7小时内，约60%给予的SG-75以SG-86的形式在尿液中回收。十二指肠内给药时，SG-75迅速吸收并以未改变的形式转移至门静脉。SG-75具有降压和冠状血管舒张作用，而SG-86对心血管系统几乎没有影响。即使大剂量（50微克/分钟或500微克/分钟）向冠状动脉灌注系统持续输注SG-86，SG-75（0.3 - 20微克冠状动脉内注射）的冠状血管舒张作用也不受影响。
