Functional pharmacology of GABAA receptors containing the chicken brain γ4 subunit

I C Forster; Robert J Harvey; M G Darlison; J A Benson

doi:10.1016/S0014-2999(01)00964-5

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Functional pharmacology of GABAA receptors containing the chicken brain γ4 subunit

Journal article

Peer reviewed

Functional pharmacology of GABAA receptors containing the chicken brain γ4 subunit

I C Forster, Robert J Harvey, M G Darlison and J A Benson

European Journal of Pharmacology, Vol.419(1), pp.1-7

2001

DOI: https://doi.org/10.1016/S0014-2999(01)00964-5

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Abstract

benzodiazepine pharmacology

electrophysiology

GABAA receptor

xenopus oocyte

Zn2+ inhibition

The functional pharmacology of receptors composed of the chicken brain GABAA receptor γ4 subunit and the mammalian GABAA receptor α3 and β2 subunits was studied by heterologous expression in Xenopus laevis oocytes using the two electrode voltage-clamp technique. GABA-evoked currents had an EC50 of 180±30 μM. Responses were blocked by the competitive and non-competitive GABAA receptor antagonists, bicuculline methochloride and picrotoxin. Sodium pentobarbital reversibly potentiated the current several-fold, and Zn2+ ions blocked the current with high potency (IC50 = 20 μM). GABA-evoked currents were potentiated by the benzodiazepine site full agonists flunitrazepam and triazolam and less by the partial agonists abecarnil and bretazenil. The inverse agonists methyl-β-carboline-3-carboxylate (β-CCM) and methyl 6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) reduced the current. However, the imidazobenzodiazepine Ro 15-4513, which acts as an inverse agonist at mammalian αxβyγ2 GABAA receptors (where x = 1, 2, 3 or 5, and y = 1, 2 or 3), acted as a positive agonist at the γ4 subunit-containing receptors. © 2001 Elsevier Science B.V.

Details

Title: Functional pharmacology of GABAA receptors containing the chicken brain γ4 subunit
Authors: I C Forster (Author) - Physiologisches Institut der Universität Zürich, Switzerland
Robert J Harvey (Author) - Institut für Zellbiochemie und Klinische Neurobiologie, Germany
M G Darlison (Author) - Institut für Zellbiochemie und Klinische Neurobiologie, Germany
J A Benson (Author) - Pharmakologisches Institut der Universität Zürich, Switzerland
Publication details: European Journal of Pharmacology, Vol.419(1), pp.1-7
Publisher: Elsevier BV
Date published: 2001
DOI: 10.1016/S0014-2999(01)00964-5
ISSN: 0014-2999
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: 99451078702621
Output Type: Journal article

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Web Of Science research areas: Pharmacology & Pharmacy

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