8-iodo-harmine | 234755-96-5

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 哈马拉生物碱
• 英文名称: 8-iodo-harmine
• 英文别名: 8-iodoharmine；8-iodo-7-methoxy-1-methyl-9H-pyrido[3,4-b]indole
• CAS: 234755-96-5
• 化学式: C₁₃H₁₁IN₂O
• 分子量: 338.148
• InChiKey: FMBKFOPHJNVRKU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  37.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  8-iodo-harmine 在 copper(I) chloride 、 sodium iodide 作用下， 以 phosphate buffer 、 乙醇 为溶剂， 反应 0.17h， 生成 8-[131I]-iodo-harmine
  参考文献：
  名称：

  Iodination, radioiodination and spectroscopic identification of β-carboline derivatives

  摘要：

  The synthesis and spectral properties (MS, and NMR) of radioiodinated beta-carbolines: 6-(I) and 8- (II) [I-131]-iodo-1-methyl-7-methoxy-beta-carboline ([I-131]-iodo-harmine), 6- (III) and 8- (IV) [I-131]-iodo-1-methyl-beta-carboline-7-ol ([I-131]-iodo-harmol), 8-[I-131]-iodo-1-methyl-7-methoxy-3,4-dihydro-beta-carboline (8-[I-131]-iodo-harmaline) (V), 8-[I-131]-iodo-3,4-dihydro-1-methyl-beta-carboline-7-ol (8-[I-131]-iodo-harmalol) (VI), 6-[I-131]-iodo-1-methyl-beta-carboline (6-[I-131]-iodo-harmane) (VII) are described. These are compounds of biological importance and can be used for brain mapping with SPECT technology.

  DOI：

  10.1002/(sici)1099-1344(199905)42:5<409::aid-jlcr195>3.0.co;2-a
• 作为产物：
  描述：

  肉叶云香碱 在 碘 、 thallium(III) trifluoroacetate 作用下， 生成 8-iodo-harmine
  参考文献：
  名称：

  A Facile High-Yield Synthesis of [10 B]-8-Dihydroxyboryl Harmine, a Potential Agent for Boron Neutron Capture Therapy

  摘要：

  不适用

  DOI：

  10.3390/50300526

文献信息

• SCREENING METHOD, PROTEIN INSTABILITY AND/OR STABILITY INDUCERS, AND PROTEIN ACTIVITY ASSESSMENT
  申请人：KYOTO UNIVERSITY

  公开号：US20150133467A1

  公开（公告）日：2015-05-14

  Provided is a screening method with which it is possible to determine the cause of a decrease or an increase in the amount of a target protein that is expressed by a cell. One or a plurality of embodiments include: conducting cultivation that includes bringing an assay cell into contact with a test substance, and measuring a relative amount (A) of the target protein in relation to an internal standard; conducting cultivation in which an assay cell is not brought into contact with a test substance, and measuring a relative amount (B) in relation to an internal standard; comparing the relative amount (A) and the relative amount (B); and, based on the comparison, selecting a candidate substance that induces instability and/or stability in the target protein. The assay cell is a cell that is able to express mRNA of the target protein and mRNA of the internal standard protein under the identical regulation of gene expression, or a cell having a means for expressing mRNA of the target protein and mRNA of the internal standard protein under the identical regulation of gene expression.

  提供了一种筛选方法，可以确定细胞表达的目标蛋白质数量减少或增加的原因。其中一种或多种实施方式包括：进行培养，将检测细胞与测试物质接触，并测量与内部标准相关的目标蛋白质的相对量(A)；进行培养，其中检测细胞未与测试物质接触，并测量与内部标准相关的相对量(B)；比较相对量(A)和相对量(B)；并根据比较选择诱导目标蛋白质不稳定性和/或稳定性的候选物质。检测细胞是能够在基因表达的相同调节下表达目标蛋白质mRNA和内部标准蛋白质mRNA的细胞，或具有在基因表达的相同调节下表达目标蛋白质mRNA和内部标准蛋白质mRNA的手段的细胞。
• COMPOUND PERTAINING TO NEUROPOIESIS AND DRUG COMPOSITION
  申请人：KYOTO UNIVERSITY

  公开号：US20160303089A1

  公开（公告）日：2016-10-20

  A composition for activating neurogenesis or the growth of neurons is provided. In one or more embodiments, a composition contains as an active ingredient a compound with a DYRK inhibitory capacity or a prodrug thereof or a pharmaceutically acceptable salt thereof. In one or more embodiments, a composition contains as an active ingredient a compound expressed by the following general formula (I) and/or (II) or prodrug thereof or a pharmaceutically acceptable salt thereof.

  提供了一种用于激活神经发生或神经元生长的组合物。在一个或多个实施例中，该组合物包含作为活性成分的具有DYRK抑制能力的化合物或其前药，或其药学上可接受的盐。在一个或多个实施例中，该组合物包含作为活性成分的符合以下一般式(I)和/或(II)的化合物，或其前药，或其药学上可接受的盐。
• Synthesis of 8-[10B]-dihydroxyboryl-harmine, a potential agent for boron neutron capture therapy
  作者：Jose A. Sintas、Norberto J. Macareno、Arturo A. Vitale

  DOI：10.1002/(sici)1099-1344(200001)43:1<97::aid-jlcr296>3.0.co;2-d

  日期：2000.1