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We evaluated the effect of the two N-trifluoroethyl benzodiazepines, quazepam and its 2-oxo metabolite SCH 15725, which possess preferential affinity for type I benzodiazepine recognition sites, on the binding of [3H] gamma-aminobutyric acid ([3H]GABA) to rat brain membrane preparations. The study also included compounds such as diazepam and N-desalkyl-2-oxoquazepam (SCH 17514), which have equal affinity for the type I and type II receptor subtypes. Binding of [3H]GABA was studied in frozen-thawed and repeatedly washed cortical membranes incubated in 20 mM KH2PO4 plus 50 mM KCl, pH 7.4, at 4 degrees C in the absence and presence of quazepam or its metabolites. Addition of 10(-6) M quazepam increased by 30% specific [3H]GABA binding; as revealed by Scatchard plot analysis, the effect was due to an increase in the total number of GABA receptors. The effect of quazepam was concentration dependent, and it was shared by its active metabolite SCH 15725. The potency of quazepam and SCH 15725 in enhancing [3H]GABA binding was similar to that of diazepam, whereas CL 218872 and SCH 17514 were less active. Moreover, the [3H]GABA binding-enhancing effect of quazepam was mediated by an occupancy of benzodiazepine receptors, because it was specifically antagonized by 5 X 10(-6) M Ro15-1788.
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
February 1989,
European journal of pharmacology,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
January 1983,
Molecular pharmacology,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
January 1993,
Psychopharmacology series,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
September 1991,
The Journal of clinical psychiatry,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
January 1988,
Life sciences,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
June 1995,
Brain research,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
August 1981,
Biochemical pharmacology,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
February 1979,
Proceedings of the National Academy of Sciences of the United States of America,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
June 1986,
Arzneimittel-Forschung,
M G Corda, and
E Sanna, and
A Concas, and
O Giorgi, and
E Ongini, and
V Nurchi, and
T Pintori, and
G Crisponi, and
G Biggio
November 1981,
Molecular pharmacology,
