Sakanashi M, Tomomatsu E, Fukai R, Oyama Y, Ueda S, Takenaka F, Higuchi M
Arzneimittelforschung. 1979;29(10):1530-3.
Effects of 2-nicotinamidoethyl nitrate (SG-75) on cardiovascular system were investigated using whole animals and isolated vascular smooth muscles of dogs and rabbits. In dogs in vivo SG-75 i.v. produced dose-dependent falls in systemic blood pressure (SBP) concomitant with increases in heart rate (HR). Hypotension by SG-75 was not affected by propranolol and atropine but slightly inhibited by diphenhydramine. Norepinephrine (NE) dose-dependently increased SBP, and SG-75 could not affect these effects of NE. In dog coronary arterial strips contracted with potassium, SG-75 produced a dose-dependent relaxation of these strips. These effects of SG-75 were not affected by propranolol and atropine, but slightly inhibited by diphenhydramine. NE dose-dependently increased the tension of helical strips prepared from rabbit femoral artery, rabbit aorta and dog coronary artery. But SG-75 could not alter these effects of NE. The results suggest that SG-75 may have not an adrenergic beta-receptor stimulating action, a muscarinic action and an adrenergic alpha-receptor blocking action, but an inconsiderable histamine-like action. Probably, a main action of SG-75 may be a nitroglycerin-like action.
利用犬和兔的整体动物及离体血管平滑肌,研究了2-烟酰胺基乙基硝酸盐(SG-75)对心血管系统的作用。在犬体内,静脉注射SG-75可使体循环血压(SBP)呈剂量依赖性下降,同时心率(HR)增加。SG-75引起的低血压不受普萘洛尔和阿托品影响,但可被苯海拉明轻微抑制。去甲肾上腺素(NE)可使SBP呈剂量依赖性升高,SG-75不影响NE的这些作用。在由钾收缩的犬冠状动脉条上,SG-75可使这些条带产生剂量依赖性舒张。SG-75的这些作用不受普萘洛尔和阿托品影响,但可被苯海拉明轻微抑制。NE可使由兔股动脉、兔主动脉和犬冠状动脉制备的螺旋条带张力呈剂量依赖性增加。但SG-75不能改变NE的这些作用。结果表明,SG-75可能不具有肾上腺素能β受体激动作用、毒蕈碱样作用和肾上腺素能α受体阻断作用,而具有不明显的组胺样作用。可能,SG-75的主要作用可能是类似硝酸甘油的作用。