Benzodiazepine GABA-ionophore receptor complex ligands showed persistent modulation of the chloride ionophore, labeled by [(35)S]TBPS, even after receptor complex extensive purification. GABA caused inhibition of [(35)S]TBPS binding, while benzodiazepine agonists increased and benzodiazepine inverse agonists decreased the specific [(35)S]TBPS binding to the purified receptor. When GABA binding sites were occupied by the neurotransmitter benzodiazepine receptor agonists and antagonists reversed their effects clonazepam in fact inhibited and ?-carboline ethyl ester increased [(35)S]TBPS binding in the presence of GABA. The antagonist flumazenil showed no effect both in the presence or absence of GABA.

[(35)S]TBPS binding to purified benzodiazepine-GABA-ionophore receptor complex: the effect of GABA on the modulation exerted by benzodiazepine site ligands.

MARTINI, CLAUDIA;GIANNACCINI, GINO;LUCACCHINI, ANTONIO
1989

Abstract

Benzodiazepine GABA-ionophore receptor complex ligands showed persistent modulation of the chloride ionophore, labeled by [(35)S]TBPS, even after receptor complex extensive purification. GABA caused inhibition of [(35)S]TBPS binding, while benzodiazepine agonists increased and benzodiazepine inverse agonists decreased the specific [(35)S]TBPS binding to the purified receptor. When GABA binding sites were occupied by the neurotransmitter benzodiazepine receptor agonists and antagonists reversed their effects clonazepam in fact inhibited and ?-carboline ethyl ester increased [(35)S]TBPS binding in the presence of GABA. The antagonist flumazenil showed no effect both in the presence or absence of GABA.
Martini, Claudia; Pacini, R; Giannaccini, Gino; Lucacchini, Antonio
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/13539
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