γ-氨基丁酸受体离子载体复合物：溴氰菊酯、滴滴涕及一些新型杀虫剂对大鼠脑膜制剂的不同作用

gamma-Aminobutyric acid receptor ionophore complexes: differential effects of deltamethrin, dichlorodiphenyltrichloroethane, and some novel insecticides in a rat brain membrane preparation.

作者信息

Lummis S C, Chow S C, Holan G, Johnston G A

出版信息

J Neurochem. 1987 Mar;48(3):689-94. doi: 10.1111/j.1471-4159.1987.tb05571.x.

DOI:10.1111/j.1471-4159.1987.tb05571.x

Abstract

The binding of [35S]t-butylbicyclophosphorothionate ([35S]TBPS), a gamma-aminobutyric acid (GABA)-activated chloride ionophore ligand; [3H]diazepam, a benzodiazepine agonist; and [3H]muscimol, a GABA receptor probe, were used to assess the effects at 100 microM of deltamethrin, dichlorodiphenyltrichloroethane (DDT), and three experimental insecticides--a DDT-pyrethroid hybrid, GH414 (cycloprothrin), and two DDT-analogues, GH266 and GH149 (EDO), on GABA receptor ionophore complexes in a rat brain membrane preparation. GH266 and GH149 were found to inhibit a greater percentage of [35S]TBPS binding than the same concentration of deltamethrin or DDT, although GH414 had little effect. GH266 and GH149 enhanced [3H]diazepam binding by nearly 200%, in contrast to the inhibitory effects of deltamethrin, DDT, and GH414. GH266 and GH149 also caused a dramatic enhancement of [3H]muscimol binding, 367 and 236% of control, respectively, whereas DDT and deltamethrin caused only a moderate enhancement. The effects of the insecticides on binding affinity and density were examined for each of the ligands. The results show a differential interaction of the insecticides on the various ligand binding sites.

摘要

[35S]叔丁基双环磷硫代酸酯（[35S]TBPS）是一种γ-氨基丁酸（GABA）激活的氯离子载体配体；[3H]地西泮是一种苯二氮䓬激动剂；[3H]蝇蕈醇是一种GABA受体探针，通过检测它们的结合情况来评估在100微摩尔浓度下溴氰菊酯、二氯二苯三氯乙烷（DDT）以及三种实验性杀虫剂——一种DDT-拟除虫菊酯杂交品种GH414（环丙菊酯）和两种DDT类似物GH266和GH149（EDO）对大鼠脑膜制剂中GABA受体离子载体复合物的影响。结果发现，GH266和GH149对[35S]TBPS结合的抑制百分比高于相同浓度的溴氰菊酯或DDT，而GH414的影响较小。与溴氰菊酯、DDT和GH414的抑制作用相反，GH266和GH149使[3H]地西泮结合增加了近200%。GH266和GH149还使[3H]蝇蕈醇结合显著增强，分别为对照的367%和236%，而DDT和溴氰菊酯仅引起适度增强。针对每种配体研究了杀虫剂对结合亲和力和密度的影响。结果表明，杀虫剂在不同配体结合位点上存在差异相互作用。