Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAA receptor

S H Zaman; Robert J Harvey; E A Barnard; M G Darlison

doi:10.1016/0014-5793(92)80711-O

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Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAA receptor

Journal article

Peer reviewed

Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAA receptor

S H Zaman, Robert J Harvey, E A Barnard and M G Darlison

FEBS Letters, Vol.307(3), pp.351-354

1992

DOI: https://doi.org/10.1016/0014-5793(92)80711-O

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Abstract

benzodiazepine

channel blocker

cyclodiene insecticide

GABAA receptor

invertebrate

lymnaea stagnalis

receptor activation

xenopus oocyte expression

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 (4â€²-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. © 1992.

Details

Title: Unusual effects of benzodiazepines and cyclodiene insecticides on an expressed invertebrate GABAA receptor
Authors: S H Zaman (Author)
Robert J Harvey (Author) - Universitat Hamburg, Germany
E A Barnard (Author)
M G Darlison (Author)
Publication details: FEBS Letters, Vol.307(3), pp.351-354
Publisher: John Wiley & Sons Ltd.
Date published: 1992
DOI: 10.1016/0014-5793(92)80711-O
ISSN: 0014-5793
Organisation Unit: School of Health; University of the Sunshine Coast, Queensland; School of Health and Sport Sciences - Legacy; Centre for Bioinnovation; School of Health and Behavioural Sciences - Legacy
Language: English
Record Identifier: 99450547202621
Output Type: Journal article

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