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

页码：2788 / 2799

页数：12

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