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.
Synthesis and Pharmacological Evaluation of Novel GABAA Subtype Receptor Ligands with Potential Anxiolytic-like and Anti-hyperalgesic Effect
Daniele, Simona;Martini, ClaudiaPenultimo
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2017-01-01
Abstract
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.File in questo prodotto:
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