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SB-277011 dihydrochloride

Cat. No.:YN1730026

  • CAS No. :1226917-67-4

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    • 产品名称: SB-277011 dihydrochloride
      CAS No.: 1226917-67-4
      Chemical Name: N-[trans-4-[2-(6-cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl]-4-quinolinecarboxamide, dihydrochloride
      Synonyms:SB-277011A dihydrochloride
      分子量:511.49
      分子式:C₂₈H₃₂Cl₂N₄O
      SMILES:O=C(C1=CC=NC2=CC=CC=C12)N[C@H]3CC[C@H](CCN4CC5=C(C=C(C#N)C=C5)CC4)CC3.[H]Cl.[H]Cl
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: SB-277011 dihydrochloride (SB-277011A dihydrochloride) 是一种有效的,选择性的,可口服的,可透过血脑屏障的dopamine D3受体拮抗剂,对 D3,D2,5-HT1B和 5-HT1D受体的pKi值分别为 8.0,6.0,<5.2 和 5.9。
      IC50和靶点:
      In Vitro:
      In Vivo:
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      Solvent & Solubility:
    • Stemp, G., Ashmeade, T., Branch, C.L., et al.Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the ratJ. Med. Chem.43(9),1878-1885(2000)

      Reavill, C., Taylor, S.G., Wood, M.D., et al.Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-AJ. Pharmacol. Exp. Ther.294(3),1154-1165(2000)

      Heidbreder, C.A., Gardner, E.L., Xi, Z.-X., et al.The role of central dopamine D3 receptors in drug addiction: a review of pharmacological evidenceBrain Res.Rev.49(1),77-105(2005)

      Carcinella, S., Drui, G., Boulet, S., et al.Implication of dopamine D3 receptor activation in the reversion of Parkinson's disease-related motivational deficitsTransl. Psychiatry4(6),e401(2014)

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