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烟碱乙酰胆碱受体作为镇痛靶点的研究进展

诸德源 王一然 蔡国君 徐添颖

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]. 药学实践与服务, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005
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]. 药学实践与服务, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005
ZHU Deyuan, WANG Yiran, CAI Guojun, XU Tianying. Advance in nicotinic acetylcholine receptors as analgesic targets[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005
Citation: ZHU Deyuan, WANG Yiran, CAI Guojun, XU Tianying. Advance in nicotinic acetylcholine receptors as analgesic targets[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005

烟碱乙酰胆碱受体作为镇痛靶点的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.005
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)

Advance in nicotinic acetylcholine receptors as analgesic targets

  • 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。
  • [1] Del Bufalo A, Cesario A, Salinaro G, et al. Alpha9 alpha10 nicotinic acetylcholine receptors as target for the treatment of chronic pain [J]. Curr Pharm Des, 2014, 20(38): 6042-6047.
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    [17] Holladay MW, Wasicak JT, Lin NH, et al. Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors [J]. J Med Chem, 1998, 41(4): 407-412.
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    [21] 刘献文, 张宗旺. 尼古丁镇痛作用机制的研究进展 [J]. 国际麻醉学与复苏杂志, 2013, 34(4): 368-370.
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    [27] Uteshev VV. The therapeutic promise of positive allosteric modulation of nicotinic receptors [J]. Eur J Pharmacol, 2014, 727: 181-185.
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  • [1] 王耀振, 徐灿, 吕顺莉, 田泾, 张东炜.  钾离子竞争性酸阻滞剂的药学特征研究进展 . 药学实践与服务, 2024, 42(7): 278-284. doi: 10.12206/j.issn.2097-2024.202306040
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烟碱乙酰胆碱受体作为镇痛靶点的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.005
    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)

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。

English Abstract

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]. 药学实践与服务, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005
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]. 药学实践与服务, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005
ZHU Deyuan, WANG Yiran, CAI Guojun, XU Tianying. Advance in nicotinic acetylcholine receptors as analgesic targets[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005
Citation: ZHU Deyuan, WANG Yiran, CAI Guojun, XU Tianying. Advance in nicotinic acetylcholine receptors as analgesic targets[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 309-312,375. doi: 10.3969/j.issn.1006-0111.2015.04.005
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