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. 2018 May 15;26(9):2475-2487.
doi: 10.1016/j.bmc.2018.04.011. Epub 2018 Apr 4.

A new class of pyrazolo[5,1-c][1,2,4]triazines as γ-aminobutyric type A (GABAA) receptor subtype ligand: synthesis and pharmacological evaluation

Gabriella Guerrini  1 , Giovanna Ciciani  2 , Simona Daniele  3 , Claudia Martini  3 , Camilla Costagli  2 , Chiara Guarino  2 , Silvia Selleri  2
Affiliations

A new class of pyrazolo[5,1-c][1,2,4]triazines as γ-aminobutyric type A (GABAA) receptor subtype ligand: synthesis and pharmacological evaluation

Gabriella Guerrini et al. Bioorg Med Chem. .

Abstract

A comparison between compounds with pyrazolo[1,5-a]pyrimidine structure (series 4-6) and pyrazolo[5,1-c][1,2,4]triazine core (series 9) as ligands at GABAA-receptor subtype, was evaluated. Moreover, for pyrazolotriazine derivatives having binding recognition, the interaction on recombinant rat α(1-3,5) GABAA receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n as α1-selective and 9h as α2-selective ligands.

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