𫫇泼西汀
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| 臨床資料 | |
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| 其他名稱 | AXS-14、PNU-165442G |
| 给药途径 | 口服 |
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| 法律規範狀態 | |
| 法律規範 |
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| 识别信息 | |
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| CAS号 | 98819-76-2  |
| PubChem CID | |
| IUPHAR/BPS | |
| ChemSpider | |
| UNII | |
| KEGG | |
| CompTox Dashboard (EPA) | |
| 化学信息 | |
| 化学式 | C19H23NO3 |
| 摩尔质量 | 313.40 g·mol−1 |
| 3D模型（JSmol） | |
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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
[编辑]- ^ 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）.
- ^ 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.
- ^ Search of esreboxetine. ClinicalTrials.gov. [2024-05-09]. （原始内容存档于2012-03-23）.
- ^ 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）.
- ^ 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.
- ^ 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.