ACTIONS OF INSECTICIDES ON THE INSECT GABA RECEPTOR COMPLEX

被引:39
作者
BERMUDEZ, I [1 ]
HAWKINS, CA [1 ]
TAYLOR, AM [1 ]
BEADLE, DJ [1 ]
机构
[1] OXFORD POLYTECH,SCH BIOL & MOLEC SCI,GIPSY LANE,HEADINGTON,OXON,ENGLAND
来源
JOURNAL OF RECEPTOR RESEARCH | 1991年 / 11卷 / 1-4期
关键词
D O I
10.3109/10799899109066401
中图分类号
Q2 [细胞生物学];
学科分类号
071009 ; 090102 ;
摘要
The actions of insecticides on the insect gamma-aminobutyric acid (GABA) receptor were investigated using [S-35]t-butylbicyclophosphorothionate ([S-35]TBPS) binding and voltage-clamp techniques. Specific binding of [S-35]TBPS to a membrane homogenate derived from the brain of Locusta migratoria locusts is characterised by a Kd value of 79.3 +/- 2.9 nM and a B(MAX) value of 1770 +/- 40 fmol/mg protein. [S-35]TBPS binding is inhibited by mM concentrations of barbiturates and benzodiazepines. In contrast dieldrin, ivermectin, lindane, picrotoxin and TBPS are inhibitors of [S-35]TBPS binding at the nanomolar range. Bicuculline, baclofen and pyrethroid insecticides have no effect on [S-35]TBPS binding. These results are similar to those obtained in electrophysiological studies of the current elicited by GABA in both Locusta and Periplaneta americana central neurones. Noise analysis of the effects of lindane, TBPS, dieldrin and picrotoxin on the cockroach GABA responses reveals that these compounds decrease the variance of the GABA-induced current but have no effect on its mean open time. All these compounds, with the exception of dieldrin, significantly decrease the conductance of GABA-evoked single current.
引用
收藏
页码:221 / 232
页数:12
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