Chemistry:Lubazodone

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Short description: Chemical compound
Lubazodone
Lubazodone.svg
Clinical data
Other namesYM-992; YM-35995
Routes of
administration		Oral
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC14H18FNO2
Molar mass251.301 g·mol−1
3D model (JSmol)
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Lubazodone (developmental code names YM-992, YM-35995) is an experimental antidepressant which was under development by Yamanouchi for the treatment for major depressive disorder in the late 1990s and early 2000s but was never marketed.[1][2][3] It acts as a serotonin reuptake inhibitor (Ki for SERT = 21 nM) and 5-HT2A receptor antagonist (Ki = 86 nM), and hence has the profile of a serotonin antagonist and reuptake inhibitor (SARI).[1][2] The drug has good selectivity against a range of other monoamine receptors, with its next highest affinities being for the α1-adrenergic receptor (Ki = 200 nM) and the 5-HT2C receptor (Ki = 680 nM).[1] Lubazodone is structurally related to trazodone and nefazodone, but is a stronger serotonin reuptake inhibitor and weaker as a 5-HT2A receptor antagonist in comparison to them and is more balanced in its actions as a SARI.[1][2] It reached phase II clinical trials for depression,[3] but development was discontinued in 2001 reportedly due to the "erosion of the SSRI market in the United States".[1]

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey". Current Topics in Medicinal Chemistry 6 (17): 1801–1823. 2006. doi:10.2174/156802606778249810. PMID 17017959. 
  2. ↑ 2.0 2.1 2.2 "Beyond SSRIs: Second-generation Reuptake Inhibitors for the Treatment of Depression". Drug Discovery for Psychiatric Disorders. Royal Society of Chemistry. 8 October 2012. pp. 193–. ISBN 978-1-84973-494-3. https://books.google.com/books?id=e3YoDwAAQBAJ&pg=PA193. 
  3. ↑ 3.0 3.1 "Lubazodone". AdisInsight. Springer Nature Switzerland AG. http://adisinsight.springer.com/drugs/800008166. 

External links



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