Litoxetine

Litoxetine
Clinical data
Other names	SL 81-0385; IXA-001
ATC code	None;
Identifiers
	IUPAC name 4-(naphthalen-2-ylmethoxy)piperidine;
CAS Number	86811-09-8;
PubChem CID	65650;
ChemSpider	59087;
UNII	9980ST005G;
ChEMBL	ChEMBL471036;
CompTox Dashboard (EPA)	DTXSID30235828 ;
Chemical and physical data
Formula	C16H19NO
Molar mass	241.334 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C3CNCCC3OCc2cc1ccccc1cc2;

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 (K_i for SERT = 7 nM) and modest 5-HT₃ receptor antagonist (K_i = 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.^[6] 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.^[6]

References[]

^ "Litoxetine - AdisInsight". adisinsight.springer.com. Retrieved 2018-08-25.
^ 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): 119–25. doi:10.1111/j.1365-2125.1995.tb05767.x. PMC 1365170. PMID 8562293.
^ Zoran Rankovic; Richard Hargreaves; Matilda Bingham (8 October 2012). Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. pp. 195–. ISBN 978-1-84973-494-3.
^ ^a ^b Progress in Drug Research. Birkhäuser. 6 December 2012. pp. 80–. ISBN 978-3-0348-8391-7.
^ 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): 139–45. doi:10.1016/0014-2999(93)90767-C. PMID 8385615.
^ ^a ^b "Litoxetine - IXALTIS - AdisInsight".

External links[]

"Litoxetine". Drug Information Portal. U.S. National Library of Medicine.

[1] "Litoxetine - AdisInsight". adisinsight.springer.com. Retrieved 2018-08-25.

[pmid8562293-2] 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): 119–25. doi:10.1111/j.1365-2125.1995.tb05767.x. PMC 1365170. PMID 8562293.

[RankovicHargreaves2012-3] Zoran Rankovic; Richard Hargreaves; Matilda Bingham (8 October 2012). Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. pp. 195–. ISBN 978-1-84973-494-3.

[Birkhäuser2012-4] Progress in Drug Research. Birkhäuser. 6 December 2012. pp. 80–. ISBN 978-3-0348-8391-7.

[pmid8385615-5] 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): 139–45. doi:10.1016/0014-2999(93)90767-C. PMID 8385615.

[AdisInsight-6] "Litoxetine - IXALTIS - AdisInsight".

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