65100-45-0

• 常用中文名：Imipramine-d6
• 常用英文名：Imipramine-d6
• CAS号：65100-45-0
• 分子式：C₁₉H₁₈D₆N₂
• 分子量：286.44400
• 相关类别： 信号通路 神经信号通路 5-羟色胺转运蛋白
• 发布时间：2017-09-02 20:11:05
• 更新时间：2024-01-10 21:28:42
• 丙咪嗪-d6是氘标记的盐酸丙咪嗪。盐酸丙咪嗪抑制5-羟色胺转运体,IC50值为32 nM。据报道,盐酸丙咪嗪可防止ASME易位,抑制MV和外泌体分泌[1][2][3][4][5]。

名称

• 英文名: 3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-bis(trideuteriomethyl)propan-1-amine
• 英文别名: Imipramine-d6

物化性质

• 密度: 1.064g/cm3
• 沸点: 403.089ºC at 760 mmHg
• 分子式: C₁₉H₁₈D₆N₂
• 分子量: 286.44400
• 闪点: 179.73ºC
• 精确质量: 286.23200
• PSA: 6.48000
• LogP: 3.94000
• 折射率: 1.575
• 储存条件: 2-8°C，密封，干燥

生物活性

• 描述: 丙咪嗪-d6是氘标记的盐酸丙咪嗪。盐酸丙咪嗪抑制5-羟色胺转运体,IC50值为32 nM。据报道,盐酸丙咪嗪可防止ASME易位,抑制MV和外泌体分泌[1][2][3][4][5]。
• 相关类别:
  研究领域 >> 神经疾病
  信号通路 >> 神经信号通路 >> 5-羟色胺转运蛋白
• 体外研究: 氢、碳和其他元素的稳定重同位素已被纳入药物分子,主要作为药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。
• 参考文献:

  [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

  [2]. Balkovetz DF, et al. Evidence for an imipramine-sensitive serotonin transporter in human placental brush-border membranes. J Biol Chem. 1989 Feb 5;264(4):2195-8.

  [3]. Yasuda S, et al. Imipramine ameliorates pain-related negative emotion via induction of brain-derived neurotrophic factor. Cell Mol Neurobiol. 2014 Nov;34(8):1199-208.

  [4]. Ramirez K, et al. Imipramine attenuates neuroinflammatory signaling and reverses stress-induced social avoidance. Brain Behav Immun. 2015 May;46:212-20.

  [5]. Erburu M, et al. Chronic mild stress and imipramine treatment elicit opposite changes in behavior and in gene expression in the mouse prefrontal cortex. Pharmacol BiochemBehav. 2015 Aug;135:227-36.

  [6]. Nagasawa M, et al. Chronic imipramine treatment differentially alters the brain and plasma amino acid metabolism in Wistar and Wistar Kyoto rats. Eur J Pharmacol. 2015 Sep 5;762:127-35.

  [7]. Tokarski K, et al. Imipramine counteracts corticosterone-induced alterations in the effects of the activation of 5-HT(7) receptors in rat hippocampus. J Physiol Pharmacol. 2009 Jun;60(2):83-8.

  [8]. Mariadelva Catalano, et al. Inhibiting extracellular vesicles formation and release: a review of EV inhibitors. J Extracell Vesicles. 2020; 9(1): 1703244.

安全

• 危害码 (欧洲): T+