Lubazodone Explained

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 = 21 nM) and 5-HT2A receptor antagonist (Ki = 86 nM), and hence has the profile of a serotonin antagonist and reuptake inhibitor (SARI). 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). 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. It reached phase II clinical trials for depression, but development was discontinued in 2001 reportedly due to the "erosion of the market in the United States".

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Notes and References

  1. Moltzen EK, Bang-Andersen B . 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 . 17017959 . 10.2174/156802606778249810 .
  2. Book: Gallagher PT . Beyond SSRIs: Second-generation Reuptake Inhibitors for the Treatment of Depression . Rankovic Z, Hargreaves R, Bingham M . Drug Discovery for Psychiatric Disorders. https://books.google.com/books?id=e3YoDwAAQBAJ&pg=PA193. 8 October 2012. Royal Society of Chemistry. 978-1-84973-494-3. 193–.
  3. Web site: Lubazodone . AdisInsight . Springer Nature Switzerland AG .