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Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAAreceptor

Zaman, Shahid H.; Harvey, Robert J.; Barnard, Eric A.; Darlison, Mark G.

Authors

Shahid H. Zaman

Robert J. Harvey

Eric A. Barnard

Mark G. Darlison



Abstract

We have previously reported [(1991) EMBO J. 10, 3239–3245] the sequence of an invertebrate γ‐aminobutyric acid (GABA) type A (GABAA) receptor polypeptide which forms homo‐oligomeric GABA‐gated, bicuculline‐sensitive, chloride‐ion channels upon heterologous expression. We now demonstrate that the benzodiazepines Ro5‐4864 (4′‐chlorodiazepam) and diazepam, that are active at mammalian peripheral benzodiazepine sites, and not those benzodiazepines specific for central sites, directly activate the homo‐oligomeric receptor and evoke larger maximal responses than those elicited by GABA. In addition, members of the cyclodiene class of insecticides block the channel of the receptor in a manner indistinguishable from that of picrotoxin.

Citation

Zaman, S. H., Harvey, R. J., Barnard, E. A., & Darlison, M. G. (1992). Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAAreceptor. FEBS Letters, 307(3), 351-354. https://doi.org/10.1016/0014-5793%2892%2980711-o

Journal Article Type Article
Acceptance Date Aug 3, 1992
Publication Date Aug 3, 1992
Deposit Date Aug 5, 2016
Publicly Available Date Nov 23, 2018
Journal FEBS Letters
Print ISSN 0014-5793
Electronic ISSN 1873-3468
Publisher Wiley
Peer Reviewed Peer Reviewed
Volume 307
Issue 3
Pages 351-354
DOI https://doi.org/10.1016/0014-5793%2892%2980711-o
Keywords Benzodiazepine, Channel blocker, Cyclodiene insecticide: Invertebrate, Lymnaea stagnalis, GABA, receptor, Receptor activation; Xenopus oocyte expression
Public URL http://researchrepository.napier.ac.uk/Output/328026
Contract Date Nov 23, 2018

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