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Pimozide

Cat. No.:YN320674

  • CAS No. :2062-78-4

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    • 产品名称: Pimozide
      CAS No.: 2062-78-4
      Chemical Name: 1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one
      Synonyms:匹莫齐特; R6238
      分子量:461.55
      分子式:C₂₈H₂₉F₂N₃O
      SMILES:O=C1NC2=CC=CC=C2N1C3CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3
      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: Pimozide 是dopamine receptor的拮抗剂,对 dopamine D2,D3 和 D1 受体的Ki值分别为 1.4 nM,2.5 nM 和 588 nM,同时对α1-adrenoceptor也有较高亲和性,Ki值为 39 nM;Pimozide 也是STAT3和STAT5的抑制剂。
      IC50和靶点: [{name:"Dopamine D2 receptor:1.4 nM (Ki)"},{name: "Dopamine D3 receptor:2.5 nM (Ki)"},{name: "Dopamine D1 receptor:588 nM (Ki)"},{name: "α1-adrenoceptor:39 nM (Ki)'}, 'STAT3', 'STAT5']
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    • Burstein, E.S., Ma, J., Wong, S., et al.Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonistJ. Pharmacol. Exp. Ther.315(3),1278-1287(2005)

      Richelson, E., and Souder, T.Binding of antipsychotic drugs to human brain receptors: Focus on newer generation compoundsLife Sci.68(1),29-39(2000)

      Roufos, I., Hay, S., and Schwarz, R.D.A structure-activity relationship study of novel phenylacetamides which are sodium channel blockersJ. Med. Chem.39(7),1514-1520(1996)

      Lau, J.F., Jeppesen, C.B., Rimvall, K., et al.Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amidesBioorg. Med. Chem. Lett.16(20),5303-5308(2006)

      Xenakis, S., and Sclafani, A.The effects of pimozide on the consumption of a palatable saccharin-glucose solution in the ratPharmacol. Biochem. Behav.15(3),435-442(1980)

      Navarro, J.F., Velasco, R., and Manzaneque, J.M.Acute and subchronic effects of pimozide on isolation-induced aggression in male miceProg. Neuropsychopharmacol. Biol. Psychiatry24(1),131-142(2000)

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