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2-对-(二甲氨基)苯乙烯基吡啶甲碘化物对兔主动脉条收缩反应的影响

[Effects of 2-[p-(dimethylamino)styryl]pyridine methiodide on contractive response of rabbit aortic strips].

作者信息

Wang X W, Zhou C M, Zhang K J

机构信息

Department of Pharmacology, Xinjiang Medical College, Urümqi, China.

出版信息

Zhongguo Yao Li Xue Bao. 1990 Jan;11(1):33-5.

PMID:2403010
Abstract

The effects of 2-[p-(dimethylamino) styryl]pyridine methiodide (DSPM) on rabbit aortic contraction induced by high K+, norepinephrine (NE) and Ca2+ were studied. On rabbit thoracic aortic strips, DSPM inhibited the contraction induced by KCl and NE in normal modified Tyrode's solution. DSPM shifted the dose-response relationships of KCl and NE to the right, and depressed their maximal responses; the pD'2 values were 5.09 and 5.16 respectively. After the strip had been exposed to Ca2(+)-free Tyrode's solution for 2 h, the NE-induced responses were further inhibited by DSPM, whereas the KCl-induced responses were not significantly affected. On depolarized vessels, the dose-response relationships of CaCl2 were also shifted to the right and their maximal responses were also depressed by DSPM, suggesting that DSPM is a non-competitive antagonist. The pD'2 value was 6.86. These results suggest that DSPM is a calcium antagonist. It not only inhibited the influx of extracellular calcium, but also has an inhibitory effect on the release of sequestered calcium in the rabbit aortic smooth muscle.

摘要

研究了2- [对-(二甲氨基)苯乙烯基]吡啶甲基碘化物(DSPM)对高钾、去甲肾上腺素(NE)和钙离子诱导的兔主动脉收缩的影响。在兔胸主动脉条上,DSPM在正常改良台氏液中抑制了氯化钾和NE诱导的收缩。DSPM使氯化钾和NE的剂量-反应关系右移,并降低了它们的最大反应;pD'2值分别为5.09和5.16。在主动脉条暴露于无钙台氏液2小时后,DSPM进一步抑制了NE诱导的反应,而氯化钾诱导的反应未受到显著影响。在去极化的血管上,氯化钙的剂量-反应关系也右移,其最大反应也被DSPM降低,表明DSPM是一种非竞争性拮抗剂。pD'2值为6.86。这些结果表明DSPM是一种钙拮抗剂。它不仅抑制细胞外钙的内流,而且对兔主动脉平滑肌中储存钙的释放也有抑制作用。

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