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Article

Modulation by the Membrane Protein TipE and Toxin Pharmacology

Jeffrey W. Warmke^*, Robert A.G. Reenan^||, Peiyi Wang^*, Su Qian^*, Joseph P. Arena, Jixin Wang, Denise Wunderler, Ken Liu, Gregory J. Kaczorowski, Lex H.T. Van der Ploeg^*, Barry Ganetzky^||, and Charles J. Cohen

From the ^* Department of Genetics and Molecular Biology, Department of Membrane Biochemistry and Biophysics, and Department of Cellular Biochemistry and Physiology, Merck Research Laboratories, Rahway, New Jersey 07065; and ^|| Laboratory of Genetics, University of Wisconsin, Madison, Wisconsin 53706

The Drosophila para sodium channel subunit was expressed in Xenopus oocytes alone and in combination with tipE, a putative Drosophila sodium channel accessory subunit. Coexpression of tipE with para results in elevated levels of sodium currents and accelerated current decay. Para/TipE sodium channels have biophysical and pharmacological properties similar to those of native channels. However, the pharmacology of these channels differs from that of vertebrate sodium channels: (a) toxin II from Anemonia sulcata, which slows inactivation, binds to Para and some mammalian sodium channels with similar affinity (K_d 10 nM), but this toxin causes a 100-fold greater decrease in the rate of inactivation of Para/TipE than of mammalian channels; (b) Para sodium channels are >10-fold more sensitive to block by tetrodotoxin; and (c) modification by the pyrethroid insecticide permethrin is >100-fold more potent for Para than for rat brain type IIA sodium channels. Our results suggest that the selective toxicity of pyrethroid insecticides is due at least in part to the greater affinity of pyrethroids for insect sodium channels than for mammalian sodium channels.

Key Words: Na⁺ channels • pyrethroid • insecticide • toxin • Xenopus oocyte

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