Benzodiazepine receptor (BZR) ligands.: 6 new 3-(2-,3- or 4-substituted benzyloxycarbonyl) derivatives of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide:: Receptor affinity and in vivo testing

被引:0
作者
Costanzo, A
Guerrini, G
Ciciani, G
Bruni, F
Costagli, C
Selleri, S
Costa, B
Martini, C
Aiello, PM
机构
[1] Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
[2] Univ Pisa, Dipartimento Psichiatria Neurobiol Farmacol & Bio, I-56126 Pisa, Italy
[3] Univ Florence, Dipartimento Farmacol Preclin & Clin Aiazzi Manci, I-50139 Florence, Italy
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of new 3-(2-, 3- or 4-substituted benzyloxycarbonyl) derivatives of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide and their binding affinities at the central benzodiazepine receptor (BZR) are reported. Among the synthesized compounds, the eater 12, having the best affinity (K-i = 1 nM), and compounds 5 and 10 were chosen for in vivo testing.
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页码:366 / 377
页数:12
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