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WS-12

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WS-12
IUPAC名
(1R,2S,5R)-N-(4-Methoxyphenyl)-5-methyl-2-(propan-2-yl)cyclohexane-1-carboxamide
识别
CAS号 68489-09-8
PubChem 11266244
ChemSpider 9441255
SMILES
 
  • C[C@@H]1CC[C@H]([C@@H](C1)C(=O)NC2=CC=C(C=C2)OC)C(C)C
性质
化学式 C18H27NO2
摩尔质量 289.41 g·mol−1
若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。

WS-12,化学式C18H27NO2,是一种含氮有机化合物,能作为离子通道TRPM8的强效选择性激动剂,与依色林相比,WS-12对TRPM8的激动剂效力略低,但其对TRPM8的选择性却高得多。[1][2][3][4][5]

参考文献

  1. ^ Bödding M, Wissenbach U, Flockerzi V. Characterisation of TRPM8 as a pharmacophore receptor. Cell Calcium. December 2007, 42 (6): 618–28. PMID 17517434. doi:10.1016/j.ceca.2007.03.005. 
  2. ^ Sherkheli MA, Vogt-Eisele AK, Bura D, Beltrán Márques LR, Gisselmann G, Hatt H. Characterization of selective TRPM8 ligands and their structure activity response (S.A.R) relationship. Journal of Pharmacy & Pharmaceutical Sciences. 2010, 13 (2): 242–53. PMID 20816009. doi:10.18433/j3n88n可免费查阅. 
  3. ^ Liu B, Fan L, Balakrishna S, Sui A, Morris JB, Jordt SE. TRPM8 is the principal mediator of menthol-induced analgesia of acute and inflammatory pain. Pain. October 2013, 154 (10): 2169–77. PMC 3778045可免费查阅. PMID 23820004. doi:10.1016/j.pain.2013.06.043. 
  4. ^ Peixoto-Neves D, Soni H, Adebiyi A. Oxidant-induced increase in norepinephrine secretion from PC12 cells is dependent on TRPM8 channel-mediated intracellular calcium elevation. Biochemical and Biophysical Research Communications. November 2018, 506 (3): 709–715. PMID 30376995. S2CID 53107273. doi:10.1016/j.bbrc.2018.10.120. 
  5. ^ Yin Y, Le SC, Hsu AL, Borgnia MJ, Yang H, Lee SY. Structural basis of cooling agent and lipid sensing by the cold-activated TRPM8 channel. Science. March 2019, 363 (6430). PMC 6478609可免费查阅. PMID 30733385. doi:10.1126/science.aav9334可免费查阅. 

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