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N-Desmethylclozapine

Cat. No.:YN321700

  • CAS No. :6104-71-8

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    • 生物活性
    • 参考文献
    • 产品名称: N-Desmethylclozapine
      CAS No.: 6104-71-8
      Chemical Name: 8-chloro-11-(1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
      Synonyms:N-去甲基氯氮平; Norclozapine; Desmethylclozapine; Normethylclozapine
      分子量:312.80
      分子式:C₁₇H₁₇ClN₄
      SMILES:ClC1=CC=C2C(N=C(N3CCNCC3)C4=CC=CC=C4N2)=C1
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
      Select Batch:
      Purity: 98%
    • 产品描述: N-Desmethylclozapine 是非典型抗精神病药 Clozapine 的主要活性代谢产物。N-Desmethylclozapine 是一种有效的、变构的部分M1受体激动剂 (EC50=115 nM),能通过 M1 受体激活增强海马 N-methyl-d-aspartate (NMDA) 受体电流。N-Desmethylclozapine 也是δ-opioid激动剂。
      IC50和靶点:
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      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • 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)

      Kuoppamäki, M., Syvälahti, E., and Hietala, J.Clozapine and N-desmethylclozapine are potent 5-HT1C receptor antagonistsEur. J. Pharmacol.245(2),179-182(1993)

      Lameh, J., Burstein, E.S., Taylor, E., et al.Pharmacology of N-desmethylclozapinePharmacol. Ther.115(2),223-231(2007)

      Odagaki, Y., Kinoshita, M., and Ota, T.Comparative analysis of pharmacological properties of xanomeline and N-desmethylclozapine in rat brain membranesJ. Psychopharmacol.30(9),896-912(2016)

      Maehara, S., Hikichi, H., and Ohta, H.Behavioral effects of N-desmethylclozapine on locomotor activity and sensorimotor gating function in mice-Possible involvement of muscarinic receptorsBrain Res.1418,111-119(2011)

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