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- W2017016573 abstract "A variety of pyrethroid insecticides and DDT analogs were surveyed to determine the effects of insecticide structure and stereochemistry on the modification of [3H]batrachotoxinin A-20-α-benzoate ([3H]BTX-B) binding to mouse brain voltage-sensitive sodium channels. For the α-cyano pyrethroids, the modification of specific [3H]BTX-B binding was qualitatively correlated with intrinsic mammalian toxicity. Whereas deltamethrin and the 2S stereoisomers of fenvalerate allosterically enhanced [3H]BTX-B binding, nontoxic isomers were either inhibitory or without effect. Similarly, DDT analogs and metabolites enhanced [3H]BTX-B binding in a manner that was correlated with mammalian toxicity. DDT, the most efficacious compound in this category, produced a greater degree of enhancement than other less toxic analogs and metabolites. In contrast, toxic noncyano pyrethroids either enhanced, inhibited, or had no effect on specific [3H]BTX-B binding in a manner that was not correlated with acute toxicity. Additional experiments were conducted to discern the mechanism of inhibition of specific [3H]BTX-B binding by certain pyrethroids. The α-R epimer of deltamethrin inhibited specific [3H]BTX-B binding with a plateau of inhibition at 40%. An equimolar mixture of deltamethrin and its α-R epimer produced only a marginal enhancement of [3H]BTX-B binding. Kinetic experiments were conducted to determine the effects of both an enhancer and an inhibitor of [3H]BTX-B binding on the rate of dissociation of the ligand-receptor complex. Deltamethrin decreased the rate of dissociation of the ligand-receptor complex by 28%, but the inhibitory enantiomer of deltamethrin increased the rate of dissociation by a factor of two. Whereas this assay system allows for the characterization of the binding of some pyrethroids to their recognition site on the sodium channel, the failure of certain toxic noncyano pyrethroids to enhance specific [3H]BTX-B binding represents a limitation in the use of this assay as a screen for intrinsic neurotoxicity." @default.
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- W2017016573 title "Structure-Activity Relationships for Pyrethroids and DDT Analogs as Modifiers of [3H]Batrachotoxinin A 20α-Benzoate Binding to Mouse Brain Sodium Channels" @default.
- W2017016573 doi "https://doi.org/10.1006/pest.1993.1015" @default.
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