| 词条 | TCS-OX2-29 |
| 释义 |
| verifiedrevid = 398756641 | IUPAC_name = (2S)-1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3,3-dimethyl-2-(pyridin-4-ylmethylamino)butan-1-one | image = TCS-OX2-29.svg | width = 240px | tradename = | legal_status = | routes_of_administration = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 4038 | CAS_number = 372523-75-6 | PubChem = 10408514 | C=23 | H=31 | N=3 | O=3 | molecular_weight = 397.509 g/mol | smiles = c3cnccc3CNC(C(C)(C)C)C(=O)N(Cc2cc1OC)CCc2cc1OC }}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] References1. ^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 & Medicinal Chemistry Letters. 2003 Dec 15;13(24):4497-9. {{PMID|14643355}} {{Hypnotics and sedatives}}{{Neuropeptide agonists and antagonists}}{{sedative-stub}}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}} 8 : Carboxamides|Orexin antagonists|Phenol ethers|Pyridines|Sedatives|Tetrahydroisoquinolines|Amines|Tert-butyl compounds |
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