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瑞诺类物质会改变蝗虫(沙漠飞蝗)肌肉中钾通道的通透性。

Ryanoids change the permeability of potassium channels of locust (Schistocerca gregaria) muscle.

作者信息

Vais H, Rucareanu C, Usherwood P N

机构信息

Department of Life Science, University of Nottingham, University Park, Nottingham NG7 2RD, UK.

出版信息

Pflugers Arch. 1996 Aug;432(4):700-7. doi: 10.1007/s004240050188.

Abstract

The plasma membrane of locust skeletal muscle contains two types of K+ channel; a maxi, Ca2+-activated 170 pS channel (BK channel) and an inward rectifier of 35 pS conductance (IK channel). The effects of ryanodine, 9,21-didehydroryanodine and 9,21-didehydroryanodol on these channels have been investigated. In the concentration domain 10(-9) M to 10(-5) M, ryanodine irreversibly induced a dose-dependent reduction of the reversal potential (Vrev) of the channel currents, measured under physiologically normal K+ and Na+ gradients, i.e. from approximately 60 mV in the absence of ryanodine to approximately 15 mV for 10(-5) M ryanodine. The alteration of K+ channel selectivity was Ca2+ independent. 9,21-Didehydroryanodine and 9,21-didehydroryanodol reduced Vrev, but only to approximately 35 mV during application of 10(-5) M of these compounds. 9,21-Didehydroryanodine also diminished the conductances of the locust K+ channels. The three ryanoids reduced Vrev of a Ca2+-activated, high-conductance channel in inside-out patches excised from mouse interosseal muscle, although the changes were in each case less pronounced than those for the locust K+ channels. Also, the action of 9,21-didehydroryanodine on mouse K+ (BK) channels was restricted to a shift of Vrev. For all three ryanoids, the IC50 coefficients (i.e. the concentration of toxin that gave a 50% reduction in Vrev) for the shifts in Vrev were similar for the locust and mouse muscle K+ channels.

摘要

蝗虫骨骼肌的质膜包含两种类型的钾通道

一种是大电导、钙激活的170 pS通道(BK通道),另一种是电导为35 pS的内向整流器(IK通道)。研究了ryanodine、9,21 - 二脱氢ryanodine和9,21 - 二脱氢ryanodol对这些通道的影响。在10⁻⁹ M至10⁻⁵ M的浓度范围内,ryanodine不可逆地引起通道电流反转电位(Vrev)剂量依赖性降低,该反转电位是在生理正常的钾离子和钠离子梯度下测量的,即在没有ryanodine时约为60 mV,对于10⁻⁵ M的ryanodine则降至约15 mV。钾通道选择性的改变与钙离子无关。9,21 - 二脱氢ryanodine和9,21 - 二脱氢ryanodol降低了Vrev,但在应用10⁻⁵ M的这些化合物时,仅降至约35 mV。9,21 - 二脱氢ryanodine还降低了蝗虫钾通道的电导。这三种ryanoids降低了从小鼠骨间肌切除的内向外膜片中钙激活的高电导通道的Vrev,尽管每种情况下的变化都比蝗虫钾通道的变化不那么明显。此外,9,21 - 二脱氢ryanodine对小鼠钾(BK)通道的作用仅限于Vrev的偏移。对于所有三种ryanoids,蝗虫和小鼠肌肉钾通道Vrev偏移的IC50系数(即导致Vrev降低50%的毒素浓度)相似。

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