The depressant scorpion neurotoxin LqqIT2 selectively modulates the insect voltage-gated sodium channel

被引:26
作者
Bosmans, F
Martin-Eauclaire, MF
Tytgat, J
机构
[1] Katholieke Univ Leuven, Fac Pharm, Toxicol Lab, B-3000 Louvain, Belgium
[2] Univ Aix Marseille 2, Inst Jean Roche, Fac Med Secteur Nord, CNRS FRE 2738, F-13916 Marseille, France
关键词
LqqIT2; depressant scorpion toxin; insecticide;
D O I
10.1016/j.toxicon.2004.12.010
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
LqqIT2 is a depressant neurotoxin present in the venom of the Leiurus quinquestriatus quinquestriatus scorpion, one of the world's most dangerous scorpions endemic to dry habitats in Africa and Asia. In order to determine its efficacy, potency and selectivity, LqqIT2 was subjected for the first time to an electrophysiological and pharmacological comparison between two different cloned sodium channels expressed in Xenopus laevis oocytes. Aside from typical beta-toxin effects, LqqIT2 also affected the inactivation process and ion selectivity of the insect voltage-gated sodium channel. The most interesting feature of LqqIT2 is its total insect-selectivity. At a concentration of 1 mu M, the insect-voltage-gated sodium channel, para, was profoundly modulated while its mammalian counterpart, the rat brain Na(v)1.2 channel, was not affected. This trait offers excellent prospects for the development of novel insecticides. (c) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:501 / 507
页数:7
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