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- W2069933440 abstract "A series of 3-substituted [1,2,4]triazino[4,3-c]benzimidazoles V were prepared and tested at the central benzodiazepine receptor (BzR). These compounds were designed as rigid analogues of the previously described N-benzylindolylglyoxylylamide derivatives IV. The title compounds V showed an affinity which depended directly on the presence of the N(10)-H group and an aromatic ring at position 3. Some of them elicited a 2- or 3-fold higher affinity with respect to that of the indolylglyoxylylamide derivatives IV (R = H). The GABA ratio and [(35)S]-tert-butylcyclophosphorothionate binding data revealed an efficacy profile of partial inverse agonists/antagonists for compounds 1c,e,f,j,k, and of a partial agonist for 2c. This last compound proved to be effective in antagonizing pentylenetetrazole-induced seizures in mice. Attempts were made to interpret the structure-affinity relationships of compounds V in the light of possible tautomeric equilibria involving the ligands." @default.
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- W2069933440 date "1999-12-10" @default.
- W2069933440 modified "2023-10-17" @default.
- W2069933440 title "3-Aryl-[1,2,4]triazino[4,3-<i>a</i>]benzimidazol-4(10<i>H</i>)-ones: Tricyclic Heteroaromatic Derivatives as a New Class of Benzodiazepine Receptor Ligands" @default.
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- W2069933440 doi "https://doi.org/10.1021/jm991131h" @default.
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