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二十二碳六烯酸对两种电压依赖性钾通道mKv1.1和mKv1.2的阻断作用

Blockade of two voltage-dependent potassium channels, mKv1.1 and mKv1.2, by docosahexaenoic acid.

作者信息

Garratt J C, McEvoy M P, Owen D G

机构信息

Wyeth Research, Taplow, Berkshire, UK.

出版信息

Eur J Pharmacol. 1996 Oct 31;314(3):393-6. doi: 10.1016/s0014-2999(96)00722-4.

Abstract

The effects of the polyunsaturated fatty acid, docosahexaenoic acid, were examined on two single cloned potassium channels, mKv1.1 and mKv1.2, stably expressed in Chinese hamster ovary cells using whole-cell patch clamp techniques. Docosahexaenoic acid produced a time- and dose-dependent, reversible block of mKv1.1 and mKv1.2. Interestingly, docosahexaenoic acid increased the rate of activation of mKv1.2 leading to an enhancement of current amplitude at short intervals following activating the voltage step. This phenomenon was not seen in the case of mKv1.1. Intracellular administration of docosahexaenoic acid did not block either type of channel. These findings suggest that docosahexaenoic acid inhibits mKv1.1 and mKv1.2 channels by acting at an extracellular site and by an open-channel blocking mechanism.

摘要

运用全细胞膜片钳技术,研究了多不饱和脂肪酸二十二碳六烯酸对稳定表达于中国仓鼠卵巢细胞中的两种单克隆钾通道mKv1.1和mKv1.2的作用。二十二碳六烯酸对mKv1.1和mKv1.2产生了时间和剂量依赖性的可逆性阻断。有趣的是,二十二碳六烯酸提高了mKv1.2的激活速率,导致在电压阶跃激活后的短时间间隔内电流幅度增强。这种现象在mKv1.1中未观察到。细胞内给予二十二碳六烯酸不会阻断任何一种通道。这些发现表明,二十二碳六烯酸通过作用于细胞外位点并通过开放通道阻断机制来抑制mKv1.1和mKv1.2通道。

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