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 pyrazolotriazines derivatives having binding recognition, the interaction on recombinant rat alpha(1-3,5) GABAA receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n as alpha1-selective and 9h as alpha2-selective ligands.
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, Giovanna Ciciani, Simona Daniele, Claudia Martini, Camilla Costagli, Chiara Guarino, Silvia Selleri. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - ELETTRONICO. - 26:(2018), pp. 2475-2487. [10.1016/j.bmc.2018.04.011]
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;Silvia Selleri
2018
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 pyrazolotriazines derivatives having binding recognition, the interaction on recombinant rat alpha(1-3,5) GABAA receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n as alpha1-selective and 9h as alpha2-selective ligands.
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