Title : Stereospecific action of pyrethroid insecticides on the gamma-aminobutyric acid receptor-ionophore complex - Lawrence_1983_Science_221_1399 |
Author(s) : Lawrence LJ , Casida JE |
Ref : Science , 221 :1399 , 1983 |
Abstract :
The potent alpha-cyano-3-phenoxybenzyl pyrethroids, including cypermethrin, deltamethrin, and fenvalerate, act stereospecifically to inhibit binding to rat brain synaptic membranes of sulfur-35-labeled t-butylbicyclophosphorothionate, a new radioligand for the picrotoxinin binding site. Scatchard analysis indicates that picrotoxinin inhibition of t-butylbicyclophosphorothionate binding is competitive whereas cypermethrin inhibition possibly involves a closely associated site in the gamma-aminobutyric acid receptor-ionophore complex. Studies with 37 pyrethroids reveal an absolute correlation, that is, no false positives or negatives, between mouse intracerebral toxicity and in vitro inhibition: all toxic cyano compounds but none of their nontoxic stereoisomers are inhibitors; cis isomers are more potent than trans isomers as both toxicants and inhibitors; and noncyano pyrethroids are much less potent or are inactive. |
PubMedSearch : Lawrence_1983_Science_221_1399 |
PubMedID: 6310756 |
Lawrence LJ, Casida JE (1983)
Stereospecific action of pyrethroid insecticides on the gamma-aminobutyric acid receptor-ionophore complex
Science
221 :1399
Lawrence LJ, Casida JE (1983)
Science
221 :1399