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Pharmaceuticals (Basel). 2017 Mar 30;10(2):37. doi: 10.3390/ph10020037.
2
Downregulations of TRPM8 expression and membrane trafficking in dorsal root ganglion mediate the attenuation of cold hyperalgesia in CCI rats induced by GFRα3 knockdown.下调背根神经节中 TRPM8 的表达和膜转运可介导 GFRα3 敲低诱导的 CCI 大鼠冷超敏反应的减弱。
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Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists.含苯并咪唑的瞬时受体电位阳离子通道亚家族 M 成员 8（TRPM8）拮抗剂的设计与优化。
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Functional interactions between transient receptor potential M8 and transient receptor potential V1 in the trigeminal system: Relevance to migraine pathophysiology.三叉神经系统中瞬时受体电位 M8 与瞬时受体电位 V1 的功能相互作用：与偏头痛发病机制的相关性。
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本文引用的文献

1
Transient Receptor Potential Channels in neuropathic pain.神经病理性疼痛中的瞬时受体电位通道
Curr Opin Pharmacol. 2017 Feb;32:9-15. doi: 10.1016/j.coph.2016.10.002. Epub 2016 Oct 27.
2
TRPM8 and Migraine.瞬时受体电位香草酸亚型8与偏头痛
Headache. 2016 Oct;56(9):1406-1417. doi: 10.1111/head.12948. Epub 2016 Sep 16.
3
High-Concentration L-Menthol Exhibits Counter-Irritancy to Neurogenic Inflammation, Thermal and Mechanical Hyperalgesia Caused by Trans-cinnamaldehyde.高浓度L-薄荷醇对反式肉桂醛引起的神经源性炎症、热痛觉过敏和机械性痛觉过敏具有抗刺激作用。
J Pain. 2016 Aug;17(8):919-29. doi: 10.1016/j.jpain.2016.05.004. Epub 2016 May 31.
4
Gene-based pleiotropy across migraine with aura and migraine without aura patient groups.基于基因的多效性在伴先兆偏头痛和无先兆偏头痛患者群体中的研究
Cephalalgia. 2016 Jun;36(7):648-57. doi: 10.1177/0333102415591497. Epub 2015 Dec 8.
5
TRPs and pain.瞬时受体电位通道与疼痛。
Semin Immunopathol. 2016 May;38(3):277-91. doi: 10.1007/s00281-015-0526-0. Epub 2015 Sep 15.
6
Functional role of the transient receptor potential melastatin 8 (TRPM8) ion channel in the urinary bladder assessed by conscious cystometry and ex vivo measurements of single-unit mechanosensitive bladder afferent activities in the rat.通过清醒膀胱测压法和大鼠离体单单位机械敏感性膀胱传入活动测量评估瞬时受体电位香草酸亚型8（TRPM8）离子通道在膀胱中的功能作用。
BJU Int. 2016 Mar;117(3):484-94. doi: 10.1111/bju.13225. Epub 2015 Aug 16.
7
Meningeal transient receptor potential channel M8 activation causes cutaneous facial and hindpaw allodynia in a preclinical rodent model of headache.在头痛的临床前啮齿动物模型中，脑膜瞬时受体电位通道M8的激活会导致面部皮肤和后爪痛觉过敏。
Cephalalgia. 2016 Feb;36(2):185-93. doi: 10.1177/0333102415584313. Epub 2015 May 5.
8
Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.发现一种对冷相关疼痛具有临床疗效的选择性瞬时受体电位香草酸亚型8（TRPM8）拮抗剂。
ACS Med Chem Lett. 2015 Jan 30;6(4):419-24. doi: 10.1021/ml500479v. eCollection 2015 Apr 9.
9
AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia.AMG2850是一种强效且具有选择性的瞬时受体电位香草酸亚型8（TRPM8）拮抗剂，在炎症性机械性超敏反应和神经性触觉异常性疼痛的大鼠模型中无效。
Naunyn Schmiedebergs Arch Pharmacol. 2015 Apr;388(4):465-76. doi: 10.1007/s00210-015-1090-9. Epub 2015 Feb 10.
10
Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist.新型2-吡啶基苯磺酰胺衍生物RQ-00203078作为一种选择性口服活性TRPM8拮抗剂的鉴定。
Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8. doi: 10.1016/j.bmcl.2014.10.074. Epub 2014 Oct 29.

用于治疗慢性疼痛和偏头痛的TRPM8拮抗剂的研发。

Development of TRPM8 Antagonists to Treat Chronic Pain and Migraine.

作者信息

Weyer Andy D, Lehto Sonya G

机构信息

Pacific University School of Physical Therapy, Hillsboro, OR 97123, USA.

One Amgen Center Dr, Thousand Oaks, CA 91320, USA.

出版信息

Pharmaceuticals (Basel). 2017 Mar 30;10(2):37. doi: 10.3390/ph10020037.

DOI:10.3390/ph10020037
PMID:28358322
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5490394/
Abstract

A review. Development of pharmaceutical antagonists of transient receptor potential melastatin 8 (TRPM8) have been pursued for the treatment of chronic pain and migraine. This review focuses on the current state of this progress.

摘要

综述。为治疗慢性疼痛和偏头痛，人们一直在研发瞬时受体电位 melastatin 8（TRPM8）的药物拮抗剂。本综述聚焦于这一进展的当前状况。