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English2-Oxoquazepam (2oxoquaz) is a novel benzodiazepine which shows preferential affinity for type I benzodiazepine recognition sites. In the present study, we analyzed the effect of gamma-aminobutyric acid (GABA), pentobarbital, and chloride ions on [3H]2oxoquaz and [3H]flunitrazepam ( [3H]FNT) binding to membrane preparations from rat and human brain. GABA stimulated [3H]-2oxoquaz and [3H]FNT binding in a concentration-dependent manner. The maximal enhancement produced by GABA on [3H]2oxoquaz binding was higher than that produced on [3H]FNT binding in both rat and human tissues. In the rat brain, the effect of GABA on [3H]2oxoquaz was similar throughout different brain areas, whereas the effect on [3H]FNT binding was lower in the cerebral cortex and hippocampus than in the cerebellum. Moreover, both [3H]2oxoquaz and [3H]FNT binding were stimulated by chloride ions and pentobarbital. The results are consistent with the hypothesis that type I benzodiazepine recognition sites are linked functionally to the GABA recognition site and the chloride ionophore.
| Autori interni: | ||
| Autori: | Corda MG; Giorgi O; Longoni B; Ongini E; Barnett A; Montaldo S; Biggio G | |
| Titolo: | gamma-Aminobutyric acid and pentobarbital enhance 2-[3H]oxoquazepam binding to type I benzodiazepine recognition sites in rat and human brain. | |
| Anno del prodotto: | 1988 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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