The Full Wiki

More info on TCS-OX2-29

TCS-OX2-29: Wikis

Advertisements

Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.

Encyclopedia

From Wikipedia, the free encyclopedia

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
Identifiers
CAS number 372523-75-6
ATC code  ?
PubChem 10408514
Chemical data
Formula C23H31N3O3 
Mol. mass 397.509 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status

TCS-OX2-29 is a drug which 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]

References

  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
Advertisements

Advertisements






Got something to say? Make a comment.
Your name
Your email address
Message