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Nortriptyline

MCE 国际站：Nortriptyline

品牌：MedChemExpress (MCE)

货号：HY-118620

CAS：72-69-5

中文名称：去甲替林

Synonyms：去甲替林; Desmethylamitriptyline; Desitriptilina

纯度：99.97%

存储条件：4°C，避光保存 *溶剂中：-80°C，6 个月；-20°C，1 个月（避光保存）

运输条件：美国大陆的室温；其他地方可能有所不同。

产品活性：ortriptyline (Desmethylamitriptyline) 是 mitriptyline 的主要活性代谢物，是一种三环类抗抑郁剂。Nortriptyline 是一种有效的自噬 (autophagy) 抑制剂，并具有抗癌作用。

生物活性： Nortriptyline (Desmethylamitriptyline) 是 Amitriptyline 的主要活性代谢产物，是一种三环类抗抑郁药，用于缓解抑郁症状。去甲替林是一种有效的自噬抑制剂^[1][2]。

体外：Amitriptyline 由 CYP2C19 代谢为活性代谢物 Nortriptyline。Nortriptyline 比血清素更能有效地阻止去甲肾上腺素的再摄取[1]。 Nortriptyline（6.25-100 μM；24-72 小时）以浓度和时间依赖性方式显着降低 TCCSUP 和小鼠 MBT-2 膀胱癌细胞的活力[3]。 Nortriptyline（12.55-100 μM；24 小时）可诱导 TCCSUP 和 MBT-2 细胞的细胞周期停滞和细胞凋亡[3]。 Nortriptyline（12.55-100 μM；24 小时）可诱导这些膀胱癌细胞的内在和外在细胞凋亡[3]。 viabilty cycle TCCSUP and MBT-2 cells[3] 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells) 24 hours Caused cell cycle arrest in these bladder cancer cells. apoptosis TCCSUP and MBT-2 cells[3] 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells) 24 hours Induced apoptosis in both TCCSUP and MBT-2 cells TCCSUP and MBT-2 cells[3] 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells) 24 hours Increased the expression of Fas, FasL, FADD, Bax, Bak, and cleaved ｆorms of caspase-3, caspase-8, caspase-9, and poly(ADP-ribose) polymerase. Decreased the expression of Bcl-2, Bcl-xL, BH3 interacting domain death agonist, X-linked inhibitor of apoptosis protein, and survivin. MCE尚未独立证实这些方法的准确性。仅供参考。

体内：Nortriptyline（10-20 mg/kg；腹腔注射；每天；持续三周）可抑制接种 MBT-2 细胞的小鼠膀胱肿瘤的生长[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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参考文献：

[1]. Dean L. Amitriptyline Therapy and CYP2D6 and CYP2C19 Genotype. In: Pratt VM, Scott SA, Pirmohamed M, et al., eds. Medical Genetics Summaries. Bethesda (MD): National Center for Biotechnology Inｆormation (US); March 23, 2017.
[2]. Petrosyan E, et al. Repurposing Autophagy Regulators in Brain Tumors [published online ahead of print, 2022 Feb 18]. Int J Cancer. 2022;10.1002/ijc.33965.
[3]. Sheau-Yun Yuan, et al. Nortriptyline induces mitochondria and death receptor-mediated apoptosis in bladder cancer cells and inhibits bladder tumor growth in vivo. Eur J Pharmacol. 2015 Aug 15:761:309-20.