Premium
Synthesis and Pharmacological Evaluation of Novel GABA A Subtype Receptor Ligands with Potential Anxiolytic‐like and Anti‐hyperalgesic Effect
Author(s) -
Guerrini Gabriella,
Ciciani Giovanna,
Crocetti Letizia,
Daniele Simona,
Ghelardini Carla,
Giovani Maria Paola,
Di Cesare Mannelli Lorenzo,
Martini Claudia,
Vergelli Claudia
Publication year - 2017
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.2882
Subject(s) - chemistry , anxiolytic , benzodiazepine , pharmacology , anxiety , receptor , gabaa receptor , combinatorial chemistry , biochemistry , psychology , psychiatry , medicine
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 GABA A ‐receptor subtype; the compound 12 was further investigated in animal models of anxiety and persistent pain.