Department of Biosciences, College of Rural and Community Development, 101D Harper Building, 810 Draanjik Drive, University of Alaska Fairbanks, Fairbanks, AK 99709-3419, USA.
Molecules. 2019 Mar 7;24(5):944. doi: 10.3390/molecules24050944.
Neuronal nicotinic acetylcholine receptors are cell membrane-bound ion channels that are widely distributed in the central nervous system. The α4β2 subtype of neuronal nicotinic acetylcholine receptor plays an important role in modulating the signaling pathways for pain. Previous studies have shown that agonists, partial agonists, and positive allosteric modulators for the α4β2 receptors are effective in relieving pain. Desformylflustrabromine is a compound that acts as an allosteric modulator of α4β2 receptors. The aim of this study was to assess the effects of desformylflustrabromine on chemically induced pain. For this purpose, the formalin-induced pain test and the acetic acid-induced writhing response test were carried out in CD-1 mice. Both tests represent chemical assays for nociception. The results show that desformylflustrabromine is effective in producing an analgesic effect in both tests used for assessing nociception. These results suggest that desformylflustrabromine has the potential to become a clinically used drug for pain relief.
神经元烟碱型乙酰胆碱受体是位于细胞膜上的离子通道，广泛分布于中枢神经系统。神经元烟碱型乙酰胆碱受体的α4β2 亚型在调节疼痛信号通路方面发挥着重要作用。先前的研究表明，α4β2 受体的激动剂、部分激动剂和正变构调节剂对缓解疼痛有效。去甲氟烷溴是一种作为α4β2 受体变构调节剂的化合物。本研究旨在评估去甲氟烷溴对化学诱导性疼痛的影响。为此，在 CD-1 小鼠中进行了福尔马林诱导的疼痛试验和醋酸诱导的扭体反应试验。这两种试验均代表了伤害感受的化学测定。结果表明，去甲氟烷溴在用于评估伤害感受的两种试验中均能有效产生镇痛作用。这些结果表明，去甲氟烷溴有可能成为一种用于缓解疼痛的临床应用药物。
