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Lubazodone

January 01, 1970

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 SERTTooltip 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 SSRITooltip selective serotonin reuptake inhibitor market in the United States".[1]

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
  • 161178-07-0 Y
PubChem CID
  • 157919
ChemSpider
  • 138947 N
UNII
  • 850TB2B172
CompTox Dashboard (EPA)
  • DTXSID30167074
Chemical and physical data
FormulaC14H18FNO2
Molar mass251.301 g·mol−1
3D model (JSmol)
  • Interactive image
  • 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
 NY (what is this?)  (verify)

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.

External links edit

  • Lubazodone - AdisInsight
 

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

January 01, 1970
lubazodone, developmental, code, names, 35995, experimental, antidepressant, which, under, development, yamanouchi, treatment, major, depressive, disorder, late, 1990s, early, 2000s, never, marketed, acts, serotonin, reuptake, inhibitor, serttooltip, serotonin. 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 SERTTooltip 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 a1 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 SSRITooltip selective serotonin reuptake inhibitor market in the United States 1 LubazodoneClinical dataOther namesYM 992 YM 35995Routes ofadministrationOralATC codeNoneIdentifiersIUPAC name 2S 2 7 fluoro 2 3 dihydro 1H inden 4 yl oxymethyl morpholineCAS Number161178 07 0 YPubChem CID157919ChemSpider138947 NUNII850TB2B172CompTox Dashboard EPA DTXSID30167074Chemical and physical dataFormulaC 14H 18F N O 2Molar mass251 301 g mol 13D model JSmol Interactive imageSMILES C1CC2 C C CC C2C1 F OC C H 3CNCCO3InChI 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 NKey HTODIQZHVCHVGM JTQLQIEISA N N N Y what is this verify References edit 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 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 a b Lubazodone AdisInsight Springer Nature Switzerland AG External links editLubazodone AdisInsight nbsp This drug article relating to the nervous system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Lubazodone amp oldid 1214861454, wikipedia, wiki, book, books, library,

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