钙诱导大鼠肾膜外周型苯二氮卓受体的调节。

D J Calvo, J H Medina
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引用次数: 0

摘要

研究了Ca2+离子对3H-RO 5-4864与外周苯二氮卓受体结合的影响。大鼠肾膜在37℃下与Ca2+预孵育产生了3H-RO 5-4864结合的剂量依赖性抑制。在0℃预孵育的膜中没有观察到抑制作用。Ca2+的作用本质上是竞争性的,并且通过添加EGTA完全逆转。在1 mM时,CaCl2的效果最大,而CoCl2和CdCl2的效果较小。没有其他二价阳离子盐检测到降低3H-RO 5-4864与大鼠肾膜的结合。总的来说,这些数据表明3H-RO 5-4864与大鼠肾膜结合的亲和力是由Ca2+调节的,并表明存在与外周苯二氮卓受体偶联的阳离子识别结合位点。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Calcium induced modulation of peripheral-type benzodiazepine receptors in rat kidney membranes.

The effects of Ca2+ ions on 3H-RO 5-4864 binding to the peripheral benzodiazepine receptor were examined. Preincubation of rat kidney membranes with Ca2+ at 37 degrees C produced a dose-dependent inhibition of 3H-RO 5-4864 binding. No inhibition was observed in membranes preincubated at 0 degrees C. The effect of Ca2+ was competitive in nature and was fully reversed by the addition of EGTA. At 1 mM, the maximal effect was achieved with CaCl2, whereas CoCl2 and CdCl2 had lesser effects. No other divalent cation salts examined decreased 3H-RO 5-4864 binding to rat kidney membranes. Collectively, these data demonstrate that the affinity of 3H-RO 5-4864 binding to rat kidney membranes is regulated by Ca2+ and suggest the presence of cation recognition binding sites coupled to the peripheral benzodiazepine receptor.

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