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]
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| Other names | YM-992; YM-35995 |
| Routes of administration | Oral |
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| Formula | C14H18FNO2 |
| Molar mass | 251.301 g·mol−1 |
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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
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