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Esreboxetine

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Esreboxetine
File:Esreboxetine.png
Systematic (IUPAC) name
(2S)-2-[(S)-(2-ethoxyphenoxy)phenylmethyl]morpholine
Clinical data
  • Uncontrolled
Oral
Identifiers
98819-76-2 7pxY
None
PubChem CID 65856
ChemSpider 59268 7pxN
UNII L8S50ZY490 7pxY
KEGG D09340 7pxY
Chemical data
Formula C19H23NO3
313.391 g/mol
 14pxN (what is this?)  (verify)

Esreboxetine is a selective norepinephrine reuptake inhibitor which was under development by Pfizer for the treatment of neuropathic pain and fibromyalgia but failed to show significant benefit over currently available medications and was discontinued.[1][2][3][4] It is the (+)-(S,S)-enantiomer of reboxetine and is even more selective in comparison.[1][5]

However, recently it has been shown that esreboxetine could be effective in fibromyalgia patients.[6]

See also

References

  1. ^ a b Matilda Bingham; Napier, Susan Jolliffe (2009). Transporters as Targets for Drugs (Topics in Medicinal Chemistry). Berlin: Springer. ISBN 3-540-87911-0. 
  2. ^ Rao SG (October 2009). "Current progress in the pharmacological therapy of fibromyalgia". Expert Opinion on Investigational Drugs 18 (10): 1479–93. PMID 19732029. doi:10.1517/13543780903203771. 
  3. ^ "Search of: esreboxetine - List Results - ClinicalTrials.gov". 
  4. ^ "Musculoskeletal Report: Pfizer Stops Work on Esreboxetine for FM". 
  5. ^ Fish, P. V.; MacKenny, M.; Bish, G.; Buxton, T.; Cave, R.; Drouard, D.; Hoople, D.; Jessiman, A.; Miller, D.; Pasquinet, C.; Patel, B.; Reeves, K.; Ryckmans, T.; Skerten, M.; Wakenhut, F. (2009). "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 50 (4): 389. doi:10.1016/j.tetlet.2008.11.025.  edit
  6. ^ Arnold, L. M., Hirsch, I., Sanders, P., Ellis, A. and Hughes, B. (2012), Safety and efficacy of esreboxetine in patients with fibromyalgia: A fourteen-week, randomized, double-blind, placebo-controlled, multicenter clinical trial. Arthritis & Rheumatism, 64: 2387–2397. doi: 10.1002/art.34390



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