The synthesis and binding study of new 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 3-ester compounds are reported. A pharmacological evaluation of the high-affinity ligands 1-4 belonging to the 3-heteroarylester series is made. The 3-(2-thienylinethoxycarbonyl) derivative 4 stands out from the other heteroarylesters and is found, using nine different behavioral methods, to be a functionally selective ligand in vivo: it shows anxiolytic-like activity in the conflict models (light-dark box and plus maze test) similarly to diazepam, without any sedative and amnesic properties or interference from alcohol.
BENZODIAZEPINE RECEPTOR LIGANDS. 7. SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NEW 3-ESTERS OF THE 8-CHLOROPYRAZOLO[5,1-C][1,2,4]BENZOTRIAZINE 5-OXIDE. 3-(2- THIENYLMETHOXYCARBONYL) DERIVATIVE: AN ANXIOSELECTIVE AGENT IN RODENTS / F. BRUNI; P. MALMBERG; A. COSTANZO; G. CICIANI; G. GUERRINI; S. SELLERI; C. COSTAGLI; C. MARTINI; B. COSTA; F. BESNARD. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - ELETTRONICO. - 45:(2002), pp. 5710-5720. [10.1021/jm020944u]
BENZODIAZEPINE RECEPTOR LIGANDS. 7. SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NEW 3-ESTERS OF THE 8-CHLOROPYRAZOLO[5,1-C][1,2,4]BENZOTRIAZINE 5-OXIDE. 3-(2- THIENYLMETHOXYCARBONYL) DERIVATIVE: AN ANXIOSELECTIVE AGENT IN RODENTS.
BRUNI, FABRIZIO;MALMBERG, PETRA;COSTANZO, ANNARELLA;CICIANI, GIOVANNA;GUERRINI, GABRIELLA;SELLERI, SILVIA;
2002
Abstract
The synthesis and binding study of new 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 3-ester compounds are reported. A pharmacological evaluation of the high-affinity ligands 1-4 belonging to the 3-heteroarylester series is made. The 3-(2-thienylinethoxycarbonyl) derivative 4 stands out from the other heteroarylesters and is found, using nine different behavioral methods, to be a functionally selective ligand in vivo: it shows anxiolytic-like activity in the conflict models (light-dark box and plus maze test) similarly to diazepam, without any sedative and amnesic properties or interference from alcohol.
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