The presence of an ionophore site was demonstrated on the benzodiazepine/GABA receptor complex purified from rat brain. [(3)H]Flunitrazepam binding to the purified receptor was enhanced by Clions and barbiturate, compounds that interact with the ionophore site. The enhancement was concentration dependent and antagonized by the convulsant drug picrotoxinin. The site was directly labelled by [(3)S]t-butylbicyclophosphorothionate, a blocking agent of the GABA-controlled ionophore channel. The binding was specific and saturable and showed a dissociation constant of 52 nM.

BARBITURATE ENHANCEMENT OF [H-3] FLUNITRAZEPAM BINDING TO PURIFIED BENZODIAZEPINE GABA RECEPTOR FROM RAT-BRAIN

MARTINI, CLAUDIA;GIANNACCINI, GINO;LUCACCHINI, ANTONIO
1987-01-01

Abstract

The presence of an ionophore site was demonstrated on the benzodiazepine/GABA receptor complex purified from rat brain. [(3)H]Flunitrazepam binding to the purified receptor was enhanced by Clions and barbiturate, compounds that interact with the ionophore site. The enhancement was concentration dependent and antagonized by the convulsant drug picrotoxinin. The site was directly labelled by [(3)S]t-butylbicyclophosphorothionate, a blocking agent of the GABA-controlled ionophore channel. The binding was specific and saturable and showed a dissociation constant of 52 nM.
1987
Martini, Claudia; Bertolini, M; Giannaccini, Gino; Lucacchini, Antonio
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/173360
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