Pharmacology of insect GABA receptors |
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| Authors: | David B Sattelle Sarah C R Lummis James F H Wong James J Rauh |
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| Institution: | (1) AFRC Laboratory of Molecular Signalling, Department of Zoology, University of Cambridge, Downing Street, CB2 3EJ Cambridge, UK;(2) Agricultural Products, E.I. du Pont de Nemours and Company, P. O. Box 80402, 19880-0402 Wilmington, Delaware, USA |
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| Abstract: | A GABA-operated Cl– channel that is bicuculline-insensitive is abundant in the nervous tissue of cockroach, in housefly head preparations and thorax/abdomen preparations, and in similar preparations from several insect species. Bicuculline-insensitive GABA-operated Cl– channels, which are rare in vertebrates, possess sites of action of benzodiazepines, steroids and insecticides that are pharmacologically-distinct from corresponding sites on vertebrate GABAA receptors. The pharmacological profile of the benzodiazepine-binding site linked to an insect CNS GABA-operated Cl– channel resembles more closely that of vertebrate peripheral benzodiazepine-binding sites. Six pregnane steroids and certain polychlorocycloalkane insecticides, which are active att-butylbicy-clophosphorothionate (TBPS)-binding sites, also differ in their effectiveness on vertebrate and insect GABA receptors. Radioligand binding and physiological studies indicate that in insects there may be subtypes of the GABA receptor. Molecular biology offers experimental approaches to understanding the basis of this diversity.Special issue dedicated to Dr. Eugene Roberts |
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| Keywords: | GABA receptor chloride channel insect physiology biochemistry molecular biology |
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