Imipramine (hydrochloride)
中文名:盐酸丙咪嗪
CAS:113-52-0
品牌:MedChemExpress (MCE)
存储条件:4°C, sealed storage, away from moisture
生物活性:Imipramine hydrochloride 是一种具有口服活性的叔胺三环类抗抑郁药。 Imipramine hydrochloride 是一种 Fascin1 抑制剂,具有抗肿瘤活性。 Imipramine hydrochloride 还抑制 5-羟色胺转运蛋白,IC50 值为 32 nM。 Imipramine hydrochloride 刺激 U-87MG 胶质瘤细胞自噬并诱导 HL-60 细胞凋亡。盐酸丙咪嗪具有神经保护和免疫调节作用[1][2][3][4] [5]。 IC50 和目标:Fascin1、血清素自噬、细胞凋亡[1][2][3][5]
IC50:32 nM(人胎盘血清素转运蛋白)。
体外:Imipramine (0.5-300 μM, 3 days) inhibits HCT-116 cell viability[1].
Imipramine (20 μM) 抑制细胞迁移 (7 h) 和侵袭 (48 h)< sup>[1].
Imipramine (50 μM, 0-240 min) 抑制 U-87MG 胶质瘤细胞中的 PI3K/Akt/mTOR 信号通路[2]。
Imipramine (60 μM, 24 h) 刺激U-87MG胶质瘤细胞自噬[2]。
Imipramine (80 μM, 24 h) 诱导HL-60细胞凋亡[3]。
体内:丙咪嗪(20 mg/kg,腹腔注射或 15 mg/kg,口服;每日一次,持续 24 天)可减弱小鼠的神经炎症信号并逆转应激诱导的社交回避[4]。
参考文献:
[1]. Alburquerque-González B, et al. New role of the antidepressant imipramine as a Fascin1 inhibitor in colorectal cancer cells. Exp Mol Med. 2020 Feb;52(2):281-292.
[2]. Jeon SH, et al. The tricyclic antidepressant imipramine induces autophagic cell death in U-87MG glioma cells. Biochem Biophys Res Commun. 2011 Sep 23;413(2):311-7.
[3]. Xia Z, et al. The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation. J Biochem Mol Toxicol. 1999;13(6):338-47.
[4]. Ramirez K, et al. Imipramine attenuates neuroinflammatory signaling and reverses stress-induced social avoidance. Brain Behav Immun. 2015 May;46:212-20.
[5]. 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.