| 3029901 |
Crofton KM, Reiter LW, Mailman RB: Pyrethroid insecticides and radioligand displacement from the GABA receptor chloride ionophore complex. Toxicol Lett. 1987 Feb;35(2-3):183-90.
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 microM. Type II pyrethroids inhibited [35S] TBPS binding to rat brain synaptosomes with Ki values ranging from 5-10 microM. The data presented here suggest that the interaction of Type II pyrethroids with the gamma-aminobutyric acid (GABA) receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site. |
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