4-Amino-N-[2-(diethylamino)ethyl]-N-methylbenzamide | 835633-80-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-Amino-N-[2-(diethylamino)ethyl]-N-methylbenzamide
• CAS: 835633-80-2
• 化学式: C₁₄H₂₃N₃O
• 分子量: 249.356
• InChiKey: GMBSYECZSOAQQE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  49.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Compositions for treating pain and pruritus
  申请人：President and Fellows of Harvard College

  公开号：EP2425858A2

  公开（公告）日：2012-03-07

  The invention features a method for inhibiting one or more voltage-gated ion channels in a cell by contacting the cell with (i) a first compound that activates a channel-forming receptor that is present on nociceptors and/or pruriceptors; and (ii) a second compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels, wherein the second compound is capable of entering nociceptors or pruriceptors through the channel-forming receptor when the receptor is activated. The invention also features a quarternary amine derivative or other permanently or transiently charged derivative of a compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels.

  本发明的特征是一种抑制细胞中一个或多个电压门控离子通道的方法，其方法是将细胞与(i) 第一种化合物接触，该化合物可激活存在于痛觉感受器和/或瘙痒感受器上的通道形成受体；和(ii)第二种化合物，它在作用于通道的内面时抑制一个或多个电压门控离子通道，但在作用于通道的外面时并不实质上抑制所述通道，其中第二种化合物在受体被激活时能够通过通道形成受体进入痛觉感受器或刺痛感受器。本发明还有一种季胺衍生物或其他永久或瞬时带电的化合物衍生物，当作用于一个或多个电压门控离子通道的内部面时，可抑制该通道，但作用于通道的外部面时，不会对上述通道产生实质性的抑制作用。
• Methods, compositions, and kits for treating pain and pruritis
  申请人：President and Fellows of Harvard College

  公开号：EP2446903A2

  公开（公告）日：2012-05-02

  The invention features a method for inhibiting one or more voltage-gated ion channels in a cell by contacting the cell with (i) a first compound that activates a channel-forming receptor that is present on nociceptors and/or pruriceptors; and (ii) a second compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels, wherein the second compound is capable of entering nociceptors or pruriceptors through the channel-forming receptor when the receptor is activated. The invention also features a quarternary amine derivative or other permanently or transiently charged derivative of a compound that inhibits one or more voltage-gated ion channels when applied to the internal face of the channels but does not substantially inhibit said channels when applied to the external face of the channels.

  本发明的特征是一种抑制细胞中一个或多个电压门控离子通道的方法，其方法是将细胞与(i) 第一种化合物接触，该化合物可激活存在于痛觉感受器和/或瘙痒感受器上的通道形成受体；和(ii)第二种化合物，它在作用于通道的内面时抑制一个或多个电压门控离子通道，但在作用于通道的外面时并不实质上抑制所述通道，其中第二种化合物在受体被激活时能够通过通道形成受体进入痛觉感受器或刺痛感受器。本发明还有一种季胺衍生物或其他永久或瞬时带电的化合物衍生物，当作用于一个或多个电压门控离子通道的内部面时，可抑制该通道，但作用于通道的外部面时，不会对上述通道产生实质性的抑制作用。
• Permanently charged sodium and calcium channel blockers as anti-inflammatory agents
  申请人：Children's Medical Center Corporation

  公开号：US10729664B2

  公开（公告）日：2020-08-04

  The invention provides compounds, compositions, methods, and kits for the treatment of neurogenic inflammation.

  本发明提供了用于治疗神经源性炎症的化合物、组合物、方法和试剂盒。
• METHODS, COMPOSITIONS, AND KITS FOR TREATING PAIN AND PRURITIS
  申请人：President and Fellows of Harvard College

  公开号：EP2101819B1

  公开（公告）日：2013-01-09
• Compositions for treating itch
  申请人：President and Fellows of Harvard College

  公开号：EP2446903B1

  公开（公告）日：2019-10-09