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水杨酸盐和两种苯甲酸盐对场刺激豚鼠输精管和心房收缩的影响。

Effects of salicylate and two benzoates on contractions of the field-stimulated guinea-pig vas deferens and atrium.

作者信息

Brasch H

出版信息

Eur J Pharmacol. 1985 Sep 24;115(2-3):155-62. doi: 10.1016/0014-2999(85)90686-7.

Abstract

Na salicylate (3.75-30 mmol/l), Na benzoate (10.5-84 mmol/l) and Na metaiodobenzoate (0.375-0.8 mmol/l) concentration dependently reduced the contractile force of the field-stimulated guinea-pig vas deferens. Contractions elicited by either noradrenaline (0.5 mmol/l) or direct muscle stimulation were also reduced while the maximum twitch response induced by KCl (160 mmol/l) was unaffected. The twitch-inhibiting potency of salicylate and the benzoates correlated to their lipophilicity. The positive inotropic effect of field stimulation of the atrium during the refractory period was not altered by the two benzoates but was reduced by Na salicylate. It is concluded that salicylate and benzoate anions are incorporated into smooth muscle cell membranes of the vas and reduce excitability. No binding seems to occur in membranes of the atrial myocardium or the sympathetic neuron terminals and salicylate or benzoate compounds do not interfere with the liberation of neurotransmitters. In addition to its influence on the cell membrane Na salicylate can diminish contractions by uncoupling oxidative phosphorylation. The use of benzoates can help to distinguish between the two effects.

摘要

水杨酸钠(3.75 - 30毫摩尔/升)、苯甲酸钠(10.5 - 84毫摩尔/升)和间碘苯甲酸钠(0.375 - 0.8毫摩尔/升)浓度依赖性地降低了场刺激豚鼠输精管的收缩力。去甲肾上腺素(0.5毫摩尔/升)或直接肌肉刺激引起的收缩也降低了,而氯化钾(160毫摩尔/升)诱导的最大抽搐反应不受影响。水杨酸盐和苯甲酸盐的抽搐抑制效力与其亲脂性相关。两种苯甲酸盐并未改变不应期内心房场刺激的正性肌力作用,但水杨酸钠降低了该作用。得出的结论是,水杨酸盐和苯甲酸盐阴离子进入输精管平滑肌细胞膜并降低兴奋性。在心房心肌细胞膜或交感神经神经元终末似乎未发生结合,水杨酸盐或苯甲酸盐化合物不干扰神经递质的释放。除了对细胞膜的影响外,水杨酸钠还可通过解偶联氧化磷酸化来减少收缩。苯甲酸盐的使用有助于区分这两种效应。

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