噁潑西汀
噁潑西汀(INN:esreboxetine;開發代號:AXS-14、PNU-165442G),或譯埃巴西汀,是一種選擇性去甲腎上腺素再攝取抑制劑。該藥物由輝瑞公司開發,用於治療神經性疼痛和纖維肌痛,但未能顯示出比目前可用藥物顯著的益處,因此已停產。[1][2][3][4]它是瑞波西汀的(S,S)-(+)-對映體。相比之下,噁潑西汀作為去甲腎上腺素再攝取抑制劑更具選擇性。[1][5]
臨床資料 | |
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其他名稱 | AXS-14、PNU-165442G |
給藥途徑 | 口服 |
ATC碼 |
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法律規範狀態 | |
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識別資訊 | |
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CAS號 | 98819-76-2 |
PubChem CID | |
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CompTox Dashboard (EPA) | |
化學資訊 | |
化學式 | C19H23NO3 |
摩爾質量 | 313.40 g·mol−1 |
3D模型(JSmol) | |
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然而,最近發現噁潑波西汀對纖維肌痛患者有效。[6]
參考資料
- ^ 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. (原始內容存檔於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]. (原始內容存檔於2012-03-23).
- ^ Kelly J. Pfizer Stops Work on Esreboxetine for FM. Musculoskeletal Report. New York, NY. 26 February 2009. (原始內容存檔於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.