TCS-OX2-29
From Self-sufficiency
| 240px | |
| 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 |
| PubChem | CID 10408514 |
| Chemical data | |
| Formula | C23H31N3O3 |
| Molar mass | 397.509 g/mol[[Script error: No such module "String".]] |
| Script error: No such module "collapsible list". | |
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
- ↑ 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
- ↑ 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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