Abstract

Isolated presynaptic nerve terminals prepared from whole rat brain were used to evaluate the action of deltamethrin on voltage-sensitive calcium channels by measuring calcium influx and endogenous glutamate release. Deltamethrin-enhanced K +-stimulated calcium influx and subsequent Ca 2+-dependent glutamate release. The effect of deltamethrin was concentration-dependent, stereospecific, blocked by ω-conotoxin MVIIC but unaltered in the presence of tetrodotoxin. These results suggest that N-type voltage-sensitive calcium channels are a site of action at the presynaptic nerve terminal. Electrophysiological studies were carried out using rat brain Ca v2.2 and β 3 subunits coexpressed in Xenopus oocytes to validate such action. Deltamethrin reduced barium peak current in a concentraion-dependent and stereospecific manner, increased the rate of activation, and prolonged the inactivation rate of this channel. These experiments support the conclusion that N-type voltage-sensitive calcium channel operation is altered by deltamethrin.

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