| 烟碱乙酰胆碱受体作为镇痛靶点的研究进展 |
| 投稿时间：2015-01-07 修订日期：2015-05-05 点此下载全文 |
| 引用本文：诸德源,王一然,蔡国君,徐添颖.烟碱乙酰胆碱受体作为镇痛靶点的研究进展[J].药学实践杂志,2015,33(4):309~312,375 |
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| 基金项目:国家自然科学基金青年科学基金项目(81102487);国家科技重大专项"重大新药创制"(2009ZX09303-002);第二军医大学教学改革重点项目(临床医学8年制课程整合-心血管系统,BMB2014016) |
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| 中文摘要:烟碱乙酰胆碱受体(nicotinic acetylcholine receptors, nAChRs)亦称神经型尼古丁受体,在中枢和外周神经系统有广泛表达。该类受体在疼痛的信号调节中发挥重要作用。近几年,人们发现以nAChRs不同亚单位作为靶点的激动剂在多种急性和慢性疼痛模型上显示良好效果,对于发展新型低成瘾性的镇痛药物具有重要的指导意义。nAChRs阳性变构调节剂为进一步提高该类药物的镇痛效能和拓展治疗窗提供了新思路。综述近几年nAChRs与镇痛研究的最新进展,并分析该领域未来的研究热点。 |
| 中文关键词:烟碱受体 镇痛 阳性变构调节剂 |
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| Advance in nicotinic acetylcholine receptors as analgesic targets |
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| Abstract:Nicotinic acetylcholine receptors (nAChRs),also known as neuronal nicotinic receptors,are widely expressed throughout the central and peripheral nervous system. nAChRs play crucial roles in pain signaling. Recently, agonists that target specific nAChR subtypes have shown substantial efficacy in a wide range of acute and chronic pain models, contributing to developing novel analgesic drugs with low drug dependence. Positive allosteric modulators offer new approaches for increasing the potency and therapeutic window of these drugs. This review summarizes the advances in nicotinic acetylcholine receptors as analgesic targets and anticipate the future directions in this field. |
| keywords:nAChRs analgesia positive allosteric modulators |
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