DOI: 10.1002/arch.940220104. Insecticide action at the GABA‐gated chloride channel: Recognition, progress, and prospects

Insecticide action at the GABA‐gated chloride channel: Recognition, progress, and prospects

10.1002/arch.940220104

Crossref journal-article

Wiley

Archives of Insect Biochemistry and Physiology (311)

Abstract

AbstractThree billion (3 × 109) pounds of hexachlorocyclohexanes, polychlorobornanes, and chlorinated cyclodienes (such as lindane, toxaphene, and endosulfan, respectively) were used to control pest insects before their mode of action was established as blocking the GABA‐gated chloride channel. With the restricted use or demise of these polychlorocycloalkanes (each ∼ 50 to ∼ 75% by weight of chlorine), the GABAergic system is for now an underutilized target of insecticide action. Newer compounds with outstanding potency at this receptor and as toxicants to houseflies are suitably‐substituted 2,6,7‐trioxabicyclo[2.2.2]‐octanes, particularly the bicycloorthobenzoates, and 1,3‐dithianes, including those with no halogenated substitutents. Picrotoxinin analogs and alkynylphenylsilatranes also act at this target but are of lower insecticidal activity. [3H]n‐Propyl‐ethynylbicycloorthobenzoate ([3H]EBOB) is for now the best radioligand for this insecticidally‐relevant binding site in insects. Macrocyclic lactones such as the avermectins and moxidectin act at a different binding site to disrupt chloride flux and they have a different spectrum of insecticidal activity and no cross resistance with cyclodienes in houseflies. The search for new insecticides has provided the incentive and probes for a better understanding of the insect GABAergic system. © 1993 Wiley‐Liss, Inc.

Bibliography

Casida, J. E. (1993). Insecticide action at the GABAâgated chloride channel: Recognition, progress, and prospects. Archives of Insect Biochemistry and Physiology, 22(1â2), 13â23. Portico.

Authors 1

John E. Casida (first)

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Dates

Type	When
Created	20 years, 6 months ago (Feb. 24, 2005, 3 a.m.)
Deposited	1 year, 11 months ago (Aug. 31, 2023, 9:29 a.m.)
Indexed	1 week ago (Aug. 21, 2025, 2:06 p.m.)
Issued	32 years, 7 months ago (Jan. 1, 1993)
Published	32 years, 7 months ago (Jan. 1, 1993)
Published Online	20 years, 6 months ago (Feb. 7, 2005)
Published Print	32 years, 7 months ago (Jan. 1, 1993)

Funders 0

None

BibTeX

@article{Casida_1993, title={Insecticide action at the GABA‐gated chloride channel: Recognition, progress, and prospects}, volume={22}, ISSN={1520-6327}, url={http://dx.doi.org/10.1002/arch.940220104}, DOI={10.1002/arch.940220104}, number={1–2}, journal={Archives of Insect Biochemistry and Physiology}, publisher={Wiley}, author={Casida, John E.}, year={1993}, month=jan, pages={13–23} }

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