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Litoxetine

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Litoxetine
Clinical data
Other namesSL 81-0385; IXA-001
ATC code
  • None
Identifiers
  • 4-(naphthalen-2-ylmethoxy)piperidine
CAS Number
PubChemCID
ChemSpider
UNII
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC16H19NO
Molar mass241.334 g·mol−1
3D model (JSmol)
  • C3CNCCC3OCc2cc1ccccc1cc2

Litoxetine (developmental code namesSL 81-0385,IXA-001) is anantidepressant which was under clinical development for the treatment ofdepression in the early 1990s but was never marketed.[1][2] It acts as apotentserotonin reuptake inhibitor (Ki forSERTTooltip serotonin transporter = 7 nM) and modest5-HT3 receptorantagonist (Ki = 315 nM).[3][4] It hasantiemetic activity, and unlike theselective serotonin reuptake inhibitors (SSRIs), appears to have a negligible incidence ofnausea andvomiting.[5] The drug is structurally related toindalpine.[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 thephase II stage for the treatment ofurinary incontinence.[1]

References

[edit]
  1. ^abc"Litoxetine - IXALTIS".AdisInsight. Springer Nature Switzerland AG. Retrieved2018-08-25.
  2. ^Fairweather DB, Patat A, Rosenzweig P, Curson VH, Dunmore C, Dubruc C, Hindmarch I (August 1995)."The psychomotor and cognitive effects of litoxetine in young and middle aged volunteers".British Journal of Clinical Pharmacology.40 (2):119–125.doi:10.1111/j.1365-2125.1995.tb05767.x.PMC 1365170.PMID 8562293.
  3. ^Gallagher PT (8 October 2012)."Beyond SSRIs: Second-generation Reuptake Inhibitors for the Treatment of Depression". In Rankovic Z, Hargreaves R, Bingham M (eds.).Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. pp. 195–.ISBN 978-1-84973-494-3.
  4. ^abOlivier B, Soudijn W, van Wijngaarden I (6 December 2012)."Serotonin, dopamine, and norepinephrine transporters". In Jucker E (ed.).Progress in Drug Research. Birkhäuser. pp. 80–.ISBN 978-3-0348-8391-7.
  5. ^Angel I, Schoemaker H, Prouteau M, Garreau M, Langer SZ (March 1993). "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.doi:10.1016/0014-2999(93)90767-C.PMID 8385615.

External links

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DATTooltip Dopamine transporter
(DRIsTooltip Dopamine reuptake inhibitors)
NETTooltip Norepinephrine transporter
(NRIsTooltip Norepinephrine reuptake inhibitors)
SERTTooltip Serotonin transporter
(SRIsTooltip Serotonin reuptake inhibitors)
VMATsTooltip Vesicular monoamine transporters
Others
5-HT1
5-HT1A
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5-HT1F
5-HT2
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5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
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