Picrotoxinin binding sites at the GABA synapse: A target for drug action

M. K. Ticku; R. W. Olsen

doi:10.1016/0361-9230(80)90036-2

Picrotoxinin binding sites at the GABA synapse: A target for drug action

M. K. Ticku, R. W. Olsen

Department of Pharmacology

Research output: Contribution to journal › Article › peer-review

13 Scopus citations

Abstract

α-Dihydropicrotoxinin (DHP), a GABA synaptic antagonist, binds to rat brain and crayfish membranes with an apparent K_D of 1-2 μ.M. Based on several lines of evidence, it appears that DHP binds to GABA-receptor-ionophore complex at a site distinct from the GABA receptor sites. A variety of centrally acting depressant and convulsant drugs which affect GABAergic transmission inhibit DHP and not GABA binding. The data suggest that DHP-sensitive site at the GABA receptor ionophores may be involved not only in drug action but in possible regulation of the chloride ionophores.

Original language	English (US)
Pages (from-to)	213-216
Number of pages	4
Journal	Brain Research Bulletin
Volume	5
Issue number	SUPPL. 2
DOIs	https://doi.org/10.1016/0361-9230(80)90036-2
State	Published - 1980

Keywords

Convulsants
Depressants
Dihydropicrotoxinin
GABA
Ionophore
Receptor

ASJC Scopus subject areas

Neuroscience(all)

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10.1016/0361-9230(80)90036-2

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title = "Picrotoxinin binding sites at the GABA synapse: A target for drug action",

abstract = "α-Dihydropicrotoxinin (DHP), a GABA synaptic antagonist, binds to rat brain and crayfish membranes with an apparent KD of 1-2 μ.M. Based on several lines of evidence, it appears that DHP binds to GABA-receptor-ionophore complex at a site distinct from the GABA receptor sites. A variety of centrally acting depressant and convulsant drugs which affect GABAergic transmission inhibit DHP and not GABA binding. The data suggest that DHP-sensitive site at the GABA receptor ionophores may be involved not only in drug action but in possible regulation of the chloride ionophores.",

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T2 - A target for drug action

AU - Ticku, M. K.

AU - Olsen, R. W.

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N2 - α-Dihydropicrotoxinin (DHP), a GABA synaptic antagonist, binds to rat brain and crayfish membranes with an apparent KD of 1-2 μ.M. Based on several lines of evidence, it appears that DHP binds to GABA-receptor-ionophore complex at a site distinct from the GABA receptor sites. A variety of centrally acting depressant and convulsant drugs which affect GABAergic transmission inhibit DHP and not GABA binding. The data suggest that DHP-sensitive site at the GABA receptor ionophores may be involved not only in drug action but in possible regulation of the chloride ionophores.

AB - α-Dihydropicrotoxinin (DHP), a GABA synaptic antagonist, binds to rat brain and crayfish membranes with an apparent KD of 1-2 μ.M. Based on several lines of evidence, it appears that DHP binds to GABA-receptor-ionophore complex at a site distinct from the GABA receptor sites. A variety of centrally acting depressant and convulsant drugs which affect GABAergic transmission inhibit DHP and not GABA binding. The data suggest that DHP-sensitive site at the GABA receptor ionophores may be involved not only in drug action but in possible regulation of the chloride ionophores.

KW - Convulsants

KW - Depressants

KW - Dihydropicrotoxinin

KW - GABA

KW - Ionophore

KW - Receptor

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ER -

Picrotoxinin binding sites at the GABA synapse: A target for drug action

Abstract

Keywords

ASJC Scopus subject areas

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