Influence of formamidines on batrachotoxin in a 20α-benzoate binding to neural membranes from pyrethroid susceptible and resistant tobacco budworm moths Heliothis virescens

C.J. Church, S.F. Abd-Elghafar, C.O. Knowles
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引用次数: 2

Abstract

1. Amitraz stimulated [3H]batrachotoxin in A 20-α-benzoate ([3H]BTX-B) binding to neural membranes from pyrethroid susceptible (S) and resistant (R) tobacco budworm moths, but N′-(2,4-xylyl)-N-methylformamidine (SN 49844) stimulated binding only with S moths.

2. Chlordimeform stimulated [3H]BTX-B binding only with R moths, and N-(4-chloro-o-tolyl)-N-methylformamidine (demethylchlordimeform) yielded no significant stimulation with either strain.

3. A mixture of amitraz and deltamethrin, a pyrethroid that previously had been shown to enhance [3H]BTX-B binding with tobacco budworm moths, also gave significant stimulation of radioligand binding with S moths.

4. When membranes were prepared from S moths at various intervals following topical application of amitraz, deltamethrin, or a mixture of amitraz and deltamethrin, biphasic stimulation of [3H]BTX-B binding was observed, with maximum enhancement occurring at 2 and 6 hr.

5. These results provided a basis for suggesting that a formamidine binding site is located on or closely associated with the sodium channel protein.

6. Whether this site is the same as the pyrethroid/DDT binding domain remains to be demonstrated; however, similarities in responses elicited by amitraz and deltamethrin alone and in combination indicate that some relationship may exist.

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甲脒对拟除虫菊酯类杀虫剂敏感和抗性烟草芽蛾神经膜上20α-苯甲酸酯中细菌毒素的影响
1. [3H] Amitraz刺激A 20-α-苯甲酸酯([3H] btxb)与拟除虫菊酯敏感(S)和抗性(R)烟草budworm moth的神经膜结合,但N ' -(2,4- xyyll)-N-甲基甲脒(SN 49844)只刺激S蛾的结合。2 .氯虫仿仅刺激[3H]BTX-B与R飞蛾结合,而N-(4-氯-o-甲苯基)-N-甲基甲脒(去甲基氯虫仿)对两种菌株均无显著刺激作用。氨基咪唑和溴氰菊酯(一种拟除虫菊酯,先前已被证明能增强[3H]BTX-B与烟草芽蛾的结合)的混合物,也能显著刺激S蛾与放射性配体的结合。在局部应用咪唑、溴氰菊酯或咪唑和溴氰菊酯的混合物后,以不同的间隔从S月蛾中制备膜,观察到[3H]BTX-B结合的双相刺激,最大增强发生在2和6小时5。这些结果为甲脒结合位点位于钠通道蛋白上或与钠通道蛋白密切相关提供了依据。该位点是否与拟除虫菊酯/滴滴涕结合结构域相同仍有待证实;然而,阿米特拉兹和溴氰菊酯单独和联合使用引起的反应相似,表明可能存在某种关系。
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