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Lubazodone

From Wikipedia, the free encyclopedia
Abandoned experimental antidepressant drug
Pharmaceutical compound
Lubazodone
Clinical data
Other namesYM-992; YM-35995
Routes of
administration 		Oral
ATC code
  • None
Identifiers
  • (2S)-2-[(7-fluoro-2,3-dihydro-1H-inden-4-yl)oxymethyl]morpholine
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C14H18FNO2
Molar mass 251.301 g·mol−1
3D model (JSmol)
  • C1CC2=C(C=CC(=C2C1)F)OC[C@@H]3CNCCO3
  • InChI=1S/C14H18FNO2/c15-13-4-5-14(12-3-1-2-11(12)13)18-9-10-8-16-6-7-17-10/h4-5,10,16H,1-3,6-9H2/t10-/m0/s1 ☒N
  • Key:HTODIQZHVCHVGM-JTQLQIEISA-N ☒N
 ☒NcheckY (what is this?)   (verify)

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 Tooltip serotonin transporter = 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 Tooltip selective serotonin reuptake inhibitor market in the United States".[1]

References

[edit ]
  1. ^ a b c d e Moltzen EK, Bang-Andersen B (2006). "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. doi:10.2174/156802606778249810. PMID 17017959.
  2. ^ a b c 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. 193–. ISBN 978-1-84973-494-3.
  3. ^ a b "Lubazodone". AdisInsight. Springer Nature Switzerland AG.
[edit ]
DAT Tooltip Dopamine transporter
(DRIs Tooltip Dopamine reuptake inhibitors)
NET Tooltip Norepinephrine transporter
(NRIs Tooltip Norepinephrine reuptake inhibitors)
SERT Tooltip Serotonin transporter
(SRIs Tooltip Serotonin reuptake inhibitors)
VMATs Tooltip Vesicular monoamine transporters
Others
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3 –7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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