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二苯胺-2-羧酸盐对大鼠骨骼肌C1-通道电导及兴奋性特征的影响。

The effect of diphenylamine-2-carboxylate on C1- channel conductance and on excitability characteristics of rat skeletal muscle.

作者信息

Camerino D C, De Luca A, Mambrini M

机构信息

Dept. of Pharmacobiology, Faculty of Pharmacy, University of Bari, Italy.

出版信息

J Pharm Pharmacol. 1989 Jan;41(1):42-5. doi: 10.1111/j.2042-7158.1989.tb06326.x.

Abstract

The effect of diphenylamine-2-carboxylate (DPC), a blocker of the C1- conductive pathway in C1- transporting epithelia, has been evaluated in-vitro on the electrophysiological variables of rat extensor digitorum longus muscle fibres. DPC (5-240 microM) caused a dose-related increase of membrane resistance which was attributed entirely to a fall in C1- channel conductance (IC50, 120 microM), since potassium conductance was not affected by the treatment. DPC also modified fibre excitability. A significant dose-dependent increase was observed in the latency of the action potential and in the excitability of the membrane. DPC was less potent on striated fibres than anthracene-9-carboxylic acid, another specific blocker of C1- channel conductance. Moreover DPC was less potent on skeletal muscle than on C1- transporting epithelia. Morphological differences in the C1- channels or of the drug binding sites may account for the differences between tissues.

摘要

二苯胺 -2- 羧酸盐(DPC)是C1 - 转运上皮细胞中C1 - 传导途径的阻滞剂,已在体外对大鼠趾长伸肌纤维的电生理变量进行了评估。DPC(5 - 240微摩尔)导致膜电阻呈剂量依赖性增加,这完全归因于C1 - 通道电导的下降(半数抑制浓度,120微摩尔),因为钾电导不受该处理的影响。DPC还改变了纤维的兴奋性。观察到动作电位的潜伏期和膜的兴奋性有显著的剂量依赖性增加。DPC对横纹肌纤维的作用比另一种C1 - 通道电导特异性阻滞剂蒽 -9- 羧酸弱。此外,DPC对骨骼肌的作用比对C1 - 转运上皮细胞的作用弱。C1 - 通道或药物结合位点的形态学差异可能解释了组织之间的差异。

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