2-烟酰胺基乙基硝酸盐（SG-75，尼可地尔）对吲哚美辛诱导的离体犬冠状动脉收缩的影响。

Effects of 2-nicotinamidoethyl nitrate (SG-75, nicorandil) on indomethacin-induced contractions of isolated dog coronary arteries.

作者信息

Sakanashi M, Takeo S, Miyamoto Y, Aniya Y, Higuchi M

出版信息

Jpn Heart J. 1983 Mar;24(2):289-95. doi: 10.1536/ihj.24.289.

DOI:10.1536/ihj.24.289

Abstract

Effects of 2-nicotinamidoethyl nitrate (SG-75) on contractile responses of dog coronary arteries to indomethacin were investigated in vitro. Indomethacin (3 X 10(-8) and 3 X 10(-7) Gm/ml) produced contractions of isolated coronary arterial strips, which were reproduced by successive administration of the drug. SG-75 (10(-5) Gm/ml) administered 5 min prior to indomethacin, significantly depressed indomethacin-induced contractions of the strips. In coronary arterial strips under potassium-contracture, SG-75 10(-8)-10(-4) Gm/ml) produced concentration-dependent relaxations, which were not affected by prior administration of indomethacin (3 X 10(-6) Gm/ml). Tranylcypromine (10(-4) Gm/ml) did not influence the relaxant responses of the strips to SG-75 (10(-8)-10(-5) Gm/ml) but significantly depressed them to SG-75 (10(-4) Gm/ml). Results indicate that large doses of SG-75 will induce a relaxant effect on isolated dog coronary arteries through activation of intravascular biosynthesis or release of prostacyclin from vascular tissues.

摘要

在体外研究了2-烟酰胺基乙基硝酸盐（SG-75）对狗冠状动脉对吲哚美辛收缩反应的影响。吲哚美辛（3×10⁻⁸和3×10⁻⁷克/毫升）可使离体冠状动脉条收缩，连续给药可重现这种收缩。在吲哚美辛给药前5分钟给予SG-75（10⁻⁵克/毫升），可显著抑制吲哚美辛诱导的冠状动脉条收缩。在钾收缩状态下的冠状动脉条中，SG-75（10⁻⁸ - 10⁻⁴克/毫升）产生浓度依赖性舒张，预先给予吲哚美辛（3×10⁻⁶克/毫升）对此无影响。反苯环丙胺（10⁻⁴克/毫升）不影响冠状动脉条对SG-75（10⁻⁸ - 10⁻⁵克/毫升）的舒张反应，但显著抑制其对SG-75（10⁻⁴克/毫升）的舒张反应。结果表明，大剂量的SG-75将通过激活血管内生物合成或从血管组织释放前列环素，对离体狗冠状动脉产生舒张作用。