Wang X W, Zhou C M, Zhang K J
Department of Pharmacology, Xinjiang Medical College, Urümqi, China.
Zhongguo Yao Li Xue Bao. 1990 Jan;11(1):33-5.
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.
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。