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

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 GABA(A)-receptor subtype, was evaluated. Moreover, for pyrazolotriazine derivatives having binding recognition, the interaction on recombinant rat alpha(1-3,5) GABA(A) receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n as alpha 1-selective and 9h as alpha 2-selective ligands. (C) 2018 Elsevier Ltd. All rights reserved.