Open Access Articles- Top Results for TCS-OX2-29


Systematic (IUPAC) name
(2S)-1-(3,4-Dihydro- 6,7-dimethoxy- 2(1H)-isoquinolinyl)- 3,3-dimethyl- 2-[(4-pyridinylmethyl)amino]- 1-butanone
Clinical data
PubChem CID 10408514
Chemical data
Formula C23H31N3O3
397.509 g/mol
 14pxY (what is this?)  (verify)

TCS-OX2-29 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX2, with an IC50 of 40nM and selectivity of around 250x for OX2 over OX1 receptors.[1] Orexin antagonists are expected to be useful for the treatment of insomnia, with subtype-selective antagonists such as TCS-OX2-29 potentially offering more specificity of action compared to non-selective orexin antagonists like almorexant.[2]


  1. ^ Hirose M, Egashira S, Goto Y, Hashihayata T, Ohtake N, Iwaasa H, Hata M, Fukami T, Kanatani A, Yamada K. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist. Bioorganic and Medicinal Chemistry Letters. 2003 Dec 15;13(24):4497-9. PMID 14643355
  2. ^ Roecker AJ, Coleman PJ. Orexin receptor antagonists: medicinal chemistry and therapeutic potential. Current Topics in Medicinal Chemistry. 2008;8(11):977-87. PMID 18673167

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