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
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Costanzo, A
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Costanzo, A
Guerrini, G
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Guerrini, G
Ciciani, G
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Ciciani, G
Bruni, F
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Bruni, F
Costagli, C
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Costagli, C
Selleri, S
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Selleri, S
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Costa, B
Martini, C
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Martini, C
Aiello, PM
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机构:Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
Aiello, PM
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[1] Univ Florence, Dipartimento Sci Farmaceut, I-50121 Florence, Italy
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.