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  • Title: Modification of nerve membrane sodium channels by the insecticide pyrethroids.
    Author: Narahashi T.
    Journal: Comp Biochem Physiol C Comp Pharmacol; 1982; 72(2):411-4. PubMed ID: 6128164.
    Abstract:
    1. The synthetic pyrethroids exert potent and selective actions on nerve membrane sodium channels. (+)-trans tetramethrin and (+)-trans allethrin cause repetitive discharges to be produced in the isolated crayfish and squid giant axons in response to a single stimulus as a result of an increase in depolarizing after-potential. 2. The latter effect is due to slowing of the sodium channel kinetics which causes a prolonged sodium current following the normal peak sodium current. 3. A kinetic model is proposed to account for the action of the pyrethroids in which the pyrethroid molecule binds to the sodium channels at both closed and open states to produce a modified open state. 4. (-)-trans and (-)-cis isomers of tetramethrin are ineffective in causing the effects, but prevent the active (+)-trans and (+)-cis isomers from exerting the effects. This stereospecificity provides us with an excellent opportunity for the study of binding sites of pyrethroids and other sodium channel modulators.
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