Development of ligands at γ-aminobutyrric acid type A (GABAA) receptor subtype as new agents for pain relief.
作者： Gabriella Guerrini , Giovanna Ciciani , Fabrizio Bruni , Silvia Selleri , Claudia Martini
DOI: 10.1016/J.BMC.2011.10.047
关键词: Chemistry 、 Potency 、 Hyperalgesia 、 Single injection 、 GABAA receptor 、 Receptor 、 Pharmacology 、 Benzodiazepine 、 Pain relief
摘要: Abstract The identification of compounds with selective anxiolytic-like effects, exerted through the benzodiazepine site on γ-aminobutyric acid type A (GABAA) receptors, and that show pronounced antihyperalgesia in several pain models, has oriented research towards development new agents for relief pain. Starting from our previously reported ligands at GABAA receptors showing we have designed aim identifying those devoid typical side effects classical benzodiazepines. Our preliminary results indicate 4, 10(±) 11 a very promising antihyperalgesic profile different animal models (peripheral mono-neuropathy, STZ-induced hyperalgesia). In particular exhibits high potency since it its protective effect starting dose 3 mg/kg po, after single injection.
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