𫫇泼西汀

𫫇泼西汀
臨床資料
其他名稱AXS-14、PNU-165442G
给药途径口服
ATC碼
  • 未分配
法律規範狀態
法律規範
  • 不受管制
识别信息
  • (2S)-2-[(S)-(2-ethoxyphenoxy)phenyl
    methyl]morpholine
CAS号98819-76-2  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)
化学信息
化学式C19H23NO3
摩尔质量313.40 g·mol−1
3D模型（JSmol（英语：JSmol））
  • CCOC1=CC=CC=C1O[C@H]([C@@H]2CNCCO2)C3=CC=CC=C3
  • InChI=1S/C19H23NO3/c1-2-21-16-10-6-7-11-17(16)23-19(15-8-4-3-5-9-15)18-14-20-12-13-22-18/h3-11,18-20H,2,12-14H2,1H3/t18-,19-/m0/s1 ☒N
  • Key:CBQGYUDMJHNJBX-OALUTQOASA-N ☒N

𫫇泼西汀（INN：esreboxetine；开发代号：AXS-14、PNU-165442G），或译埃巴西汀，是一种选择性去甲肾上腺素再摄取抑制剂。该药物由辉瑞公司开发，用于治疗神经性疼痛和纤维肌痛，但未能显示出比目前可用药物显着的益处，因此已停产。[1][2][3][4]它是瑞波西汀的(S,S)-(+)-对映体。相比之下，𫫇泼西汀作为去甲肾上腺素再摄取抑制剂更具选择性。[1][5]

然而，最近发现𫫇泼波西汀对纤维肌痛患者有效。[6]

参考资料

  1. ^ 1.0 1.1 Bingham M, Napier SJ. Transporters as Targets for Drugs (Topics in Medicinal Chemistry). Berlin: Springer. 2009 [2024-05-09]. ISBN 978-3-540-87911-4. （原始内容存档于2024-05-09）. 
  2. ^ Rao SG. Current progress in the pharmacological therapy of fibromyalgia. Expert Opinion on Investigational Drugs. October 2009, 18 (10): 1479–1493. PMID 19732029. S2CID 12726987. doi:10.1517/13543780903203771. 
  3. ^ Search of esreboxetine. ClinicalTrials.gov. [2024-05-09]. （原始内容存档于2012-03-23）. 
  4. ^ Kelly J. Pfizer Stops Work on Esreboxetine for FM. Musculoskeletal Report. New York, NY. 26 February 2009. （原始内容存档于29 February 2012）. 
  5. ^ Fish PV, Mackenny M, Bish G, Buxton T, Cave R, Drouard D, et al. Enantioselective synthesis of (R)- and (S)-N-Boc-morpholine-2-carboxylic acids by enzyme-catalyzed kinetic resolution: application to the synthesis of reboxetine analogs. Tetrahedron Letters. 2009, 50 (4): 389–391. doi:10.1016/j.tetlet.2008.11.025. 
  6. ^ Arnold LM, Hirsch I, Sanders P, Ellis A, Hughes B. Safety and efficacy of esreboxetine in patients with fibromyalgia: a fourteen-week, randomized, double-blind, placebo-controlled, multicenter clinical trial. Arthritis and Rheumatism. July 2012, 64 (7): 2387–2397. PMID 22275142. doi:10.1002/art.34390.