Synthesis and pharmacological evaluation of novel GABAA subtype receptor ligands with potential anxiolytic-like and anti-hyperlagesic effect

The identification of selective benzodiazepine site ligands, endowed with anxiolytic and anti-hyperalgesic action, is a relevant opportunity for the treatment of pain syndromes. Previously, we selected a compound with a promising anti-hyperalgesic profile, the 3-iodo-8-benzylaminopyrazolo [5,1-c][1,2,4]benzotriazine 5-oxide. Aimed to verify the structure–activity relationship, the corresponding 7-arylakylamino derivatives were synthesized. Compounds were tested for their affinity at GABAA-receptor subtype; the compound 12 was further investigated in animal models of anxiety and persistent pain