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EnglishA series of 2-phenyl[1,2,3]triazolo[1,2-α][1,2,4]benzotriazin-1,5(6H) -diones (PTBTs), VII, were prepared and tested at the central benzodiazepine receptor (BzR). The skeleton of these B compounds was designed by formally combining the N-C=O moieties of the known BzR ligands, triazoloquinoxalines (IV) and triazinobenzimidazoles (ATBIs) (VI). Most of the PTBTs displayed submicromolar/nanomolar potency at the BzR. The 9-chloro derivatives (45-49) were generally found to be more potent than their 9-unsubstituted counterparts (37-44). Compound 45 turned out to be the most potent of the PTBTs (K i 2.8 nM). A subset of compounds (37, 42, 45, 49), when tested for their affinity on recombinant rat α1β2γ2, α2β 2γ2, and α5β3γ2 GABA A/Bz receptor subtypes, showed enhanced affinities for the α1β2γ2 isoform, with compounds 45 and 49 exhibiting the highest selectivity. Moreover, compounds 45 and 49 were found to display a full agonist efficacy profile at α1 and α2 receptor subtypes, and an antagonist efficacy at B α5-containing receptors
| Autori interni: | ||
| Autori: | PRIMOFIORE G; FEDERICO DA SETTIMO; SABRINA TALIANI; SILVIA SALERNO; ETTORE NOVELLINO; GIOVANNI GRECO; BARBARA COSIMELLI; FRANOIS BESNARD; BARBARA COSTA; MARINA MONTALI; CLAUDIA MARTINI. | |
| Titolo: | High Affinity Central Benzodiazepine Receptor Ligands: Synthesis and Biological Evaluation of a Series of Phenyltriazolobenzotriazindione Derivatives (PTBTs) | |
| Anno del prodotto: | 2005 | |
| Digital Object Identifier (DOI): | 10.1021/jm0408722 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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