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Discovery of (S)-N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist.
Qiao, Yue; Zhang, Yang; Qiao, Zhenrui; He, Wenya; Chen, Yingda; Song, Depu; Wang, Guohao; Guo, Ning; Shao, Lulian; Tian, Zhiyong; Wang, Qiang; Yan, Lin; Qian, Hai.
Affiliation
  • Qiao Y; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Zhang Y; State Key Laboratory of Natural Medicines, Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu, 210009, China; Faculty of Biological Science and Technology, Changzhi University, 73 East Chengbei Street, Changzhi, Shanxi, 046011, China.
  • Qiao Z; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • He W; Henan-Macquarie University Joint Centre for Biomedical Innovation, School of Life Sciences, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Chen Y; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Song D; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Wang G; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Guo N; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Shao L; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Tian Z; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China.
  • Wang Q; School of Pharmaceutical Sciences, South-Central University For Nationalities, 182 Minyuan road, Wuhan, Hubei, 430074, China.
  • Yan L; School of Pharmacy, Henan University, N. Jinming Ave., Kaifeng, Henan, 475004, China. Electronic address: yanlin@henu.edu.cn.
  • Qian H; State Key Laboratory of Natural Medicines, Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, Jiangsu, 210009, China. Electronic address: qianhai24@cpu.edu.cn.
Eur J Med Chem ; 233: 114191, 2022 Apr 05.
Article in En | MEDLINE | ID: mdl-35263708
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Full text: 1 Database: MEDLINE Main subject: Capsaicin / TRPV Cation Channels Type of study: Prognostic_studies Language: En Journal: Eur J Med Chem Year: 2022 Type: Article Affiliation country: China
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Full text: 1 Database: MEDLINE Main subject: Capsaicin / TRPV Cation Channels Type of study: Prognostic_studies Language: En Journal: Eur J Med Chem Year: 2022 Type: Article Affiliation country: China