地帕明 | 303-54-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 中文名称: 地帕明
• 中文别名: 百里拉明
• 英文名称: 3-(5H-dibenzo[b,f]azepin-5-yl)-N,N-dimethylpropan-1-amine
• 英文别名: imipramine；(3-dibenzo[b,f]azepin-5-yl-propyl)-dimethyl-amine；5-<3-Dimethylaminopropyl>-5H-dibenzazepin；5-(3'-Dimethyl-amino-propyl)-5H-dibenzazepin；5-(8-Dimethylaminopropyl)-iminostilben；Depramine；3-benzo[b][1]benzazepin-11-yl-N,N-dimethylpropan-1-amine
• CAS: 303-54-8
• 化学式: C₁₉H₂₂N₂
• 分子量: 278.397
• InChiKey: AFBYHZACPPSJKD-UHFFFAOYSA-N

物化性质

• 熔点：
  56-57 °C(Solv: pentane (109-66-0))
• 沸点：
  411.21°C (rough estimate)
• 密度：
  0.9702 (rough estimate)
• 保留指数：
  1981

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  6.5
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

制备方法与用途

Depramine（GP 31406）是一种具有药理活性的三环类抗抑郁药，它能够抑制乙酰胆碱酯酶、Mg(^{2+})-ATP酶和Na+/K+ATP酶的活性。

反应信息

• 作为产物：
  描述：

  亚氨基芪 生成 地帕明
  参考文献：
  名称：

  VIEL, C.;MARCOT, B.;REDEUILH, G.;CHERQUI, J.;DJIANE, A.

  摘要：

  DOI：

文献信息

• Diagnostic/therapeutic agents
  申请人：Klaveness Jo

  公开号：US20050002865A1

  公开（公告）日：2005-01-06

  Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.

  可定位的诊断和/或治疗活性剂，例如超声对比剂，包括悬浮在水载体液中的报告物，该报告物包含含气体或生成气体的材料，该剂能够与目标形成至少两种结合对。
• Controlled absorption water-soluble pharmaceutically active organic compound formulation for once-daily administration
  申请人：Counts David F.

  公开号：US10463611B2

  公开（公告）日：2019-11-05

  The present disclosure provides a once-daily water-soluble pharmaceutically active formulation for oral administration. In certain embodiments, the composition comprises a water-soluble pharmaceutically active organic compound incorporated into a small particulate, each particulate having a core of the water-soluble pharmaceutically active organic compound or an acceptable salt thereof in reversible association with a pharmaceutically acceptable drug-binding polymer. The core of the composition being surrounded by an insoluble water permeable membrane that is capable of delaying the dissolution of the pharmaceutically active compound therewithin and providing for extended release of the pharmaceutically active compound. In some embodiments, the formulation of the invention are designed to extend release of the pharmaceutically active organic compound for about 3 hours to about 8 hours, thereby enabling preparation of an extended release formulation for any pharmaceutically active compound with a half-life of from about 16 hours to about 21 hours.

  本公开提供了一种用于口服的每日一次水溶性药用活性制剂。在某些实施方案中，该组合物包括掺入小颗粒中的水溶性药用活性有机化合物，每个颗粒都有一个水溶性药用活性有机化合物或其可接受盐的核心，该核心与药学上可接受的药物结合聚合物可逆结合。组合物的核心由不溶性透水膜包围，该膜能够延迟其中的药用活性化合物的溶解，并延长药用活性化合物的释放时间。在某些实施方案中，本发明的制剂可将药用活性有机化合物的释放时间延长约 3 小时至约 8 小时，从而能够制备半衰期为约 16 小时至约 21 小时的任何药用活性化合物的缓释制剂。
• A Focused Library of Psychotropic Analogues with Neuroprotective and Neuroregenerative Potential
  作者：Elisa Uliassi、Luis Emiliano Peña-Altamira、Aixa V. Morales、Francesca Massenzio、Sabrina Petralla、Michele Rossi、Marinella Roberti、Loreto Martinez Gonzalez、Ana Martinez、Barbara Monti、Maria Laura Bolognesi

  DOI：10.1021/acschemneuro.8b00242

  日期：2019.1.16

  Overcoming the lack of effective treatments and the continuous clinical trial failures in neurodegenerative drug discovery might require a shift from the prevailing paradigm targeting pathogenesis to the one targeting simultaneously neuroprotection and neuroregeneration. In the studies reported herein, we sought to identify small molecules that might exert neuroprotective and neuroregenerative potential as tools against neurodegenerative diseases. In doing so, we started from the reported neuroprotective/neuroregenerative mechanisms of psychotropic drugs featuring a tricyclic alkylamine scaffold. Thus, we designed a focused-chemical library of 36 entries aimed at exploring the structural requirements for efficient neuroprotective/neuroregenerative cellular activity, without the manifestation of toxicity. To this aim, we developed a synthetic protocol, which overcame the limited applicability of previously reported procedures. Next, we evaluated the synthesized compounds through a phenotypic screening pipeline, based on primary neuronal systems. Phenothiazine 2Bc showed improved neuroregenerative and neuroprotective properties with respect to reference drug desipramine (2Aa). Importantly, we have also shown that 2Bc outperformed currently available drugs in cell models of Alzheimer's and Parkinson's diseases and attenuates microglial activation by reducing iNOS expression.
• <i>N</i>-Dimethylaminopropylation in a Solid-Liquid Two Phase System: Synthesis of Chlorpromazine, its Analogs, and Related Compounds
  作者：S. J. Schmolka、Hans Zimmer

  DOI：10.1055/s-1984-30719

  日期：——
• SCHMOLKA, S. J.;ZIMMER, H., SYNTHESIS, BRD, 1984, N 1, 29-31
  作者：SCHMOLKA, S. J.、ZIMMER, H.

  DOI：——

  日期：——