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EnglishThe synthesis and the binding study of new 3-arylesters and 3-heteroarylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 8-substituted are reported. The nature of these substituents (in terms of lipophilic and electronic features) seems to influence the binding affinity. High-affinity ligands were studied in mice in vivo for their pharmacological effects, considering six potential benzodiazepine actions: anxiolytic-like effects, muscle relaxant effects, motor coordination, anticonvulsant action, spontaneous motor activity, and ethanol-potentiating action. Compounds 4d and 6d showed an inverse-agonist profile. These compounds were evaluated also for their binding at benzodiazepine site on GABAA receptor complex (GABAA/BzR complex) subtype to evaluate their subtype selectivity.
| Autori interni: | |
| Autori: | GUERRINI G; COSTANZO A; CICIANI G; BRUNI F; SELLERI S; COSTAGLI C; BESNARD; F; COSTA B; MARTINI C; DE SIENA G; MALMBERG-AIELLO P. |
| Titolo: | Benzodiazepine receptor ligands. 8: Synthesis and pharmacological evaluation of new pyrazolo[5,1-c] [1,2,4]benzotriazine 5-oxide 3- and 8-disubstituted: High affinity ligands endowed with inverse-agonist pharmacological efficacy |
| Anno del prodotto: | 2006 |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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http://hdl.handle.net/11568/205178
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