Convulsant/depressant site of action at the allosteric benzodiazepine-gaba receptor-ionophore complex

Maharaj K. Ticku, G. Maksay

Research output: Contribution to journalArticle

131 Citations (Scopus)

Abstract

Several classes of centrally acting convulsant, depressant, anticonvulsant and anxiolytic drugs modulate GABAergic transmission. The post-synaptic receptor with which these drugs interact in an allosteric complex with distinct binding sites for GABA, benzodiazepines, picrotoxinin and related compounds. Convulsants which inhibit GABA transmission (except bicuculline) inhibit competitively the binding of dihydropicrotoxinin (DHP) or t-butylbicyclophosphorothionate (TBPT) to the picrotoxinin site and prevent the allosteric enhancing effect of depressant drugs on GABA and benzodiazepine binding. Depressant drugs give a mixed inhibition of TBPT binding. The possible topography of the picrotoxinin site and its relationship to convulsant/depressant drug action at the benzodiazepine-GABA receptor-ionophore complex is discussed.

Original languageEnglish
Pages (from-to)2363-2375
Number of pages13
JournalLife Sciences
Volume33
Issue number24
DOIs
Publication statusPublished - Dec 12 1983

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Convulsants
Ionophores
GABA-A Receptors
gamma-Aminobutyric Acid
Benzodiazepines
Pharmaceutical Preparations
Allosteric Site
Neurotransmitter Receptor
Bicuculline
Anti-Anxiety Agents
Anticonvulsants
Binding Sites
Topography
picrotoxinin
tert-butylbicyclophosphorothionate

ASJC Scopus subject areas

  • Pharmacology

Cite this

Convulsant/depressant site of action at the allosteric benzodiazepine-gaba receptor-ionophore complex. / Ticku, Maharaj K.; Maksay, G.

In: Life Sciences, Vol. 33, No. 24, 12.12.1983, p. 2363-2375.

Research output: Contribution to journalArticle

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