z-logo
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.

This content is not available in your region!

Continue researching here.

Having issues? You can contact us here