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Volume 271, Number 33, Issue of August 16, 1996 pp. 20187-20191
©1996 by The American Society for Biochemistry and Molecular Biology, Inc.

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Identification of a Drosophila melanogaster Glutamate-gated Chloride Channel Sensitive to the Antiparasitic Agent Avermectin

(Received for publication, April 15, 1996, and in revised form, May 30, 1996)

From the Department of Genetics and Molecular Biology and the ^§ Department of Cellular Biochemistry and Physiology, Merck Research Laboratories, Rahway, New Jersey 07065-0900

Glutamate-gated chloride channels, members of the ligand-gated ion channel superfamily, have been shown in nematodes and in insects to be a target of the antiparasitic agent avermectin. Two subunits of the Caenorhabditis elegans glutamate-gated chloride channel have been cloned: GluCl- and GluCl-. We report the cloning of a Drosophila melanogaster glutamate-gated chloride channel, DrosGluCl-, which shares 48% amino acid and 60% nucleotide identity with the C. elegans GluCl channels. Expression of DrosGluCl- in Xenopus oocytes produces a homomeric chloride channel that is gated by both glutamate and avermectin. The DrosGluCl- channel has several unique characteristics not observed in C. elegans GluCl: dual gating by avermectin and glutamate, a rapidly desensitizing glutamate response, and a lack of potentiation of the glutamate response by avermectin. The pharmacological data support the hypothesis that the DrosGluCl- channel represents the arthropod H-receptor and an important target for the avermectin class of insecticides.

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