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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
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC14H18FNO2
Molar mass251.301 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 namesYM-992,YM-35995) is an experimentalantidepressant which was under development byYamanouchi for the treatment formajor depressive disorder in the late 1990s and early 2000s but was never marketed.[1][2][3] It acts as aserotonin reuptake inhibitor (Ki forSERTTooltip serotonin transporter = 21 nM) and5-HT2A receptorantagonist (Ki = 86 nM), and hence has the profile of aserotonin antagonist and reuptake inhibitor (SARI).[1][2] The drug has goodselectivity against a range of othermonoamine receptors, with its next highestaffinities being for theα1-adrenergic receptor (Ki = 200 nM) and the5-HT2C receptor (Ki = 680 nM).[1] Lubazodone is structurally related totrazodone andnefazodone, 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 reachedphase IIclinical trials for depression,[3] but development was discontinued in 2001 reportedly due to the "erosion of theSSRITooltip selective serotonin reuptake inhibitor market in the United States".[1]

References

[edit]
  1. ^abcdeMoltzen 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. ^abcGallagher 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. ^ab"Lubazodone".AdisInsight. Springer Nature Switzerland AG.

External links

[edit]
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
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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