Synthesis and Pharmacological Evaluation of Novel GABAA Subtype Receptor Ligands with Potential Anxiolytic-like and Anti-hyperalgesic Effect

被引：5
|
作者：
Guerrini, Gabriella [1 ]
Ciciani, Giovanna [1 ]
Crocetti, Letizia [1 ]
Daniele, Simona [3 ]
Ghelardini, Carla [2 ]
Giovannoni, Maria Paola [1 ]
Mannelli, Lorenzo Di Cesare [2 ]
Martini, Claudia [3 ]
Vergelli, Claudia [1 ]
机构：
[1] Univ Firenze, Dipartimento NEUROFARBA, Sez Farmaceut Nutraceut, Florence, Italy
[2] Univ Firenze, Dipartimento NEUROFARBA, Sez Farmacol, Florence, Italy
[3] Univ Pisa, Dipartimento FARM, Pisa, Italy
来源：
JOURNAL OF HETEROCYCLIC CHEMISTRY | 2017年 / 54卷 / 05期
关键词：
BENZODIAZEPINE-RECEPTOR; PAIN; RAT; MODULATION; EFFICACY; ACID;
D O I：
10.1002/jhet.2882
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
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.
引用
收藏
页码：2788 / 2799
页数：12
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