Ogata N, Vogel S M, Narahashi T
Department of Pharmacology, Northwestern University Medical School, Chicago, Illinois 60611.
FASEB J. 1988 Oct;2(13):2895-900. doi: 10.1096/fasebj.2.13.2458984.
Effects of deltamethrin, a pyrethroid insecticide, and lindane, the gamma isomer of hexachlorocyclohexane, on the gamma-aminobutyric acid (GABA)-activated ion channels were studied using cultured neurons isolated from the newborn rat dorsal root ganglia. The neuron was voltage clamped using the whole cell patch clamp technique. Two components of inward chloride currents were generated in response to bath application of GABA. One of the components was selectively blocked by 1 x 10(-5)M lindane in a stereospecific manner, but neither component was affected by 1 x 10(-5)M deltamethrin, which drastically prolonged the voltage-activated sodium channel current. Thus, the action of lindane to stimulate the nervous system is partly because of an interaction with the GABA receptor-channel complex. The target site of deltamethrin is not the GABA receptor-channel complex but the sodium channel. The results suggest a multiplicity of the GABAA receptor-chloride channel complex.
使用从新生大鼠背根神经节分离的培养神经元，研究了拟除虫菊酯类杀虫剂溴氰菊酯和六氯环己烷的γ异构体林丹对γ-氨基丁酸（GABA）激活的离子通道的影响。采用全细胞膜片钳技术对神经元进行电压钳制。浴槽施加GABA可产生两种内向氯化物电流成分。其中一种成分被1×10⁻⁵M林丹以立体特异性方式选择性阻断，但两种成分均不受1×10⁻⁵M溴氰菊酯影响，溴氰菊酯可显著延长电压激活的钠通道电流。因此，林丹刺激神经系统的作用部分是由于与GABA受体-通道复合物相互作用。溴氰菊酯的作用靶点不是GABA受体-通道复合物，而是钠通道。结果提示GABAA受体-氯化物通道复合物具有多样性。
