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-hyperlagesic effect / Guerrini, Gabriella; Ciciani, Giovanna; Crocetti, Letizia; Daniele, Simona; Ghelardini, Carla; Giovannoni, Maria Paola; Lorenzo Di Cesare Mannelli, ; Martini, Claudia; Vergelli, Claudia. - In: JOURNAL OF HETEROCYCLIC CHEMISTRY. - ISSN 1943-5193. - ELETTRONICO. - 54:(2017), pp. 2788-2799. [10.1002/jhet.2882]

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

GUERRINI, GABRIELLA;CICIANI, GIOVANNA;CROCETTI, LETIZIA;GHELARDINI, CARLA;GIOVANNONI, MARIA PAOLA;DI CESARE MANNELLI, LORENZO;VERGELLI, CLAUDIA
2017

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
2017
54
2788
2799
Guerrini, Gabriella; Ciciani, Giovanna; Crocetti, Letizia; Daniele, Simona; Ghelardini, Carla; Giovannoni, Maria Paola; Lorenzo Di Cesare Mannelli, ; ...espandi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1080951
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