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局部麻醉药:一类新型的线粒体ATP酶部分抑制剂。

Local anesthetics: a new class of partial inhibitors of mitochondrial ATPase.

作者信息

Adade A B, Chignell D, Vanderkooi G

出版信息

J Bioenerg Biomembr. 1984 Dec;16(5-6):353-63. doi: 10.1007/BF00743231.

Abstract

The following characteristics are reported for mitochondrial ATPase prepared by the chloroform extraction method: (1) The pH optimum for enzyme activity is at 8.0. (2) The neutral anesthetic benzocaine inhibits the enzyme at all pH values. (3) Reciprocal plots of 1/v versus 1/[ATP] show that inhibition by lidocaine, tetracaine, dibucaine, and chlorpromazine is noncompetitive; slope and intercept replots are hyperbolic, showing that the inhibition is partial rather than complete.

摘要

以下是通过氯仿萃取法制备的线粒体ATP酶的特性:(1)酶活性的最适pH值为8.0。(2)中性麻醉剂苯佐卡因在所有pH值下均抑制该酶。(3)1/v对1/[ATP]的倒数作图表明,利多卡因、丁卡因、地布卡因和氯丙嗪的抑制作用是非竞争性的;斜率和截距重作图呈双曲线,表明抑制是部分性的而非完全性的。

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