Imipramine 是一种具有口服活性的叔胺类三环抗抑郁药。Imipramine 是一种具有抗肿瘤活性的Fascin1抑制剂。Imipramine 也抑制 5-羟色胺转运体 (serotonin transporter)，其IC50值为 32 nM。Imipramine 刺激 U-87MG 胶质瘤细胞自噬（autophagy），诱导 HL-60 细胞凋亡（apoptosis）。Imipramine 具有神经保护和免疫调节作用。
| 生物活性 | Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is aFascin1inhibitor with antitumor activities. Imipramine also inhibitsserotonin transporterwith anIC50value of 32 nM. Imipramine stimulates U-87MG glioma cellsautophagyand induces HL-60 cellapoptosis. Imipramine shows neuroprotective and immunomodulatory effects[1][2][3][4][5]. |
| IC50& Target | Fascin1, Serotonin Transporter, Autophagy, Apoptosis[1][2][3][5]
IC50: 32 nM (human placental serotonin transporter)[5] |
体外研究
(In Vitro) | Imipramine (0.5-300 μM, 3 days) inhibits HCT-116 cell viability[1].
Imipramine (20 μM) inhibits cell migration (7 h) and invasion (48 h)[1].
Imipramine (50 μM, 0-240 min) inhibites the PI3K/Akt/mTOR signaling pathway in U-87MG glioma cells[2].
Imipramine (60 μM, 24 h) stimulates U-87MG glioma cells autophagy[2].
Imipramine (80 μM, 24 h) induces HL-60 cell apoptosis[3].
Cell Viability Assay[1] | Cell Line: | DLD-1, HCT-116, and SW-480 | | Concentration: | 0.5-300 μM | | Incubation Time: | 3 days | | Result: | Inhibited cell viability and HCT-116 was more sensitive than DLD-1 and SW-480. |
Cell Migration Assay[1] | Cell Line: | DLD-1, HCT-116, and SW-480 | | Concentration: | 20 μM | | Incubation Time: | 7 h | | Result: | Produced a remarkable inhibition of migration in all assayed cell lines. |
Cell Invasion Assay[1] | Cell Line: | HCT-116 | | Concentration: | 20 μM | | Incubation Time: | 48 h | | Result: | Inhibited cell invasion through Matrigel. |
Western Blot Analysis[2] | Cell Line: | U-87MG | | Concentration: | 50 μM | | Incubation Time: | 0, 15, 30, 60, 120 and 240 min | | Result: | Markedly inhibited the phosphorylation of both Akt (Ser473) and mTOR (Ser2481) in a time-dependent manner. Also dephosphorylated p70 S6K, a downstream target of mTOR. |
Cell Autophagy Assay[2] | Cell Line: | U-87MG | | Concentration: | 60 μM | | Incubation Time: | 24 h | | Result: | Stimulated the induction of autophagy through the redistribution of LC3 in U-87MG glioma cells. |
Apoptosis Analysis[3] | Cell Line: | HL-60 | | Concentration: | 80 μM | | Incubation Time: | 24 h | | Result: | Induced cell apoptosis. |
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体内研究
(In Vivo) | Imipramine (20 mg/kg, i.p. or 15 mg/kg, p.o.; daily for 24 days) attenuates neuroinflammatory signaling and reverses stress-induced social avoidance in mice[4].
| Animal Model: | Male C57BL/6 mice (6–8 weeks old) subjected to RSD (repeated social defeat) and HCC (home cage control)[4] | | Dosage: | 20 mg/kg or 15 mg/kg | | Administration: | Intraperitoneal injection or oral administration, daily for 24 days | | Result: | Reversed RSD-induced social avoidance behavior, significantly increasing the interaction time, significantly decreased stress-induced mRNA levels for IL-6 in brain microglia. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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