||Pyrethroid Insecticides and Radioligand Displacement from the GABA Receptor Chloride Ionophore Complex.
Crofton, K. M. ;
Reiter, L. W. ;
Mailman, R. B. ;
||Health Effects Research Lab., Research Triangle Park, NC. ;North Carolina Univ. at Chapel Hill.
Hazardous materials ;
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Radioligand binding displacement studies were conducted to determine the effects of Type I and II pyrethroids on (3H)-flunitrazepam (FLU), (3H)-muscimol (MUS), and (35S)t-butylbicyclophosphorothionate (TBPS) binding. Competition experiments with (3H)-FLU and (3H)-MUS indicate a lack of competition for binding by the pyrethroids. Type I pyrethroids failed to compete for the binding of (35S)-TBPS at concentrations as high as 50 pM. Type II pyrethroids inhibited (35S)-TBPS binding to rat brain synaptosomes with Ki values ranging from 5-10 pM. The data presented here suggest that the interaction of Type II pyrethroids with the GABA receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.