Chemistry:Litoxetine

From HandWiki
Short description: Chemical compound
Litoxetine
Litoxetine-2D-skeletal.png
Clinical data
Other namesSL 81-0385; IXA-001
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC16H19NO
Molar mass241.334 g·mol−1
3D model (JSmol)

Litoxetine (developmental code names SL 81-0385, IXA-001) is an antidepressant which was under clinical development for the treatment of depression in the early 1990s but was never marketed.[1][2] It acts as a potent serotonin reuptake inhibitor (Ki for SERT = 7 nM) and modest 5-HT3 receptor antagonist (Ki = 315 nM).[3][4] It has antiemetic activity, and unlike the selective serotonin reuptake inhibitors (SSRIs), appears to have a negligible incidence of nausea and vomiting.[5] The drug is structurally related to indalpine.[4] Development of litoxetine for depression was apparently ceased in the late 1990s.[1] However, as of March 2017, development of litoxetine has been reinitiated and the drug is now in the phase II stage for the treatment of urinary incontinence.[1]

References

  1. ↑ 1.0 1.1 1.2 "Litoxetine - IXALTIS" (in en). AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800001264. 
  2. ↑ "The psychomotor and cognitive effects of litoxetine in young and middle aged volunteers". British Journal of Clinical Pharmacology 40 (2): 119–125. August 1995. doi:10.1111/j.1365-2125.1995.tb05767.x. PMID 8562293. 
  3. ↑ "Beyond SSRIs: Second-generation Reuptake Inhibitors for the Treatment of Depression". Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. 8 October 2012. pp. 195–. ISBN 978-1-84973-494-3. https://books.google.com/books?id=e3YoDwAAQBAJ&pg=PA195. 
  4. ↑ 4.0 4.1 "Serotonin, dopamine, and norepinephrine transporters". Progress in Drug Research. Birkhäuser. 6 December 2012. pp. 80–. ISBN 978-3-0348-8391-7. https://books.google.com/books?id=-d8FCAAAQBAJ&pg=PA80. 
  5. ↑ "Litoxetine: a selective 5-HT uptake inhibitor with concomitant 5-HT3 receptor antagonist and antiemetic properties". European Journal of Pharmacology 232 (2–3): 139–145. March 1993. doi:10.1016/0014-2999(93)90767-C. PMID 8385615. 

External links



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