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新型冠状血管扩张剂N-(2-羟乙基)烟酰胺硝酸盐(SG-75)的药效学和代谢研究

Pharmacodynamic and metabolism studies on a new coronary vasodilator, N-(2-hydroxyethyl) nicotinamide nitrate (SG-75).

作者信息

Sakai K, Ohba Y, Akima M, Kamiyama H, Hinohara Y, Nakano H

出版信息

Jpn J Pharmacol. 1980 Dec;30(6):881-90. doi: 10.1254/jjp.30.881.

Abstract

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).

摘要

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。

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