Abstract:
:The 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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Guerrini G,Costanzo A,Ciciani G,Bruni F,Selleri S,Costagli C,Besnard F,Costa B,Martini C,De Siena G,Malmberg-Aiello Pdoi
10.1016/j.bmc.2005.08.058subject
Has Abstractpub_date
2006-02-01 00:00:00pages
758-75issue
3eissn
0968-0896issn
1464-3391pii
S0968-0896(05)00836-9journal_volume
14pub_type
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