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[枸橼酸3,6-二甲氨基二苯并碘杂鎓(I-65)对豚鼠乳头肌的负性肌力作用]

[Negative inotropic effect of 3,6-dimethamidodibenzopyriodonium citrate (I-65) on guinea pig papillary muscles].

作者信息

Cui Y, Tan Y H

出版信息

Zhongguo Yao Li Xue Bao. 1989 Jan;10(1):54-7.

PMID:2816402
Abstract

The effects of 3,6-dimethamidodibenzopyriodonium citrate (I-65) on the contractile response of electrically paced guinea pig papillary muscles in vitro were studied. I-65 (0.1-300 mumol/L) decreased the contractile force and inhibited isoprenaline-induced restoration of the contractile response in papillary muscles rendered inexcitable by KCl 22 mmol/L. Both effects were concentration-dependent, and the IC50 were 36.0 and 7.3 mumol/L, respectively. I-65 antagonized the positive inotropic effects of Iso and CaCl2 in a non-competitive manner. Like verapamil, I-65 had a frequency-dependent negative inotropic effect, and delayed the recovery of post-rest potentiation. It is concluded that the negative inotropic effect of I-65 results not only from the reduction of Ca2+-influx through the sarcolemmal membrane, but also from the inhibition of Ca2+ translocation in the sarcoplasmic reticulum.

摘要

研究了柠檬酸3,6 - 二甲氨基二苯并吡啶鎓(I - 65)对体外电刺激豚鼠乳头肌收缩反应的影响。I - 65(0.1 - 300 μmol/L)可降低收缩力,并抑制异丙肾上腺素诱导的由22 mmol/L氯化钾使乳头肌失去兴奋性后收缩反应的恢复。两种效应均呈浓度依赖性,IC50分别为36.0和7.3 μmol/L。I - 65以非竞争性方式拮抗异丙肾上腺素和氯化钙的正性肌力作用。与维拉帕米一样,I - 65具有频率依赖性负性肌力作用,并延迟了静息后增强的恢复。得出结论,I - 65的负性肌力作用不仅源于通过肌膜的钙内流减少,还源于对肌浆网中钙转运的抑制。

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