Nortriptyline (Synonyms: 去甲替林; Desmethylamitriptyline; Desitriptilina)

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Nortriptyline  (Synonyms: 去甲替林; Desmethylamitriptyline; Desitriptilina)

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。

Nortriptyline                                          (Synonyms: 去甲替林; Desmethylamitriptyline;  Desitriptilina)

Nortriptyline Chemical Structure

CAS No. : 72-69-5

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生物活性

Nortriptyline (Desmethylamitriptyline), the main active metabolite of Amitriptyline, is a tricyclic antidepressant. Nortriptyline is a potent autophagy inhibitor and has anticancer effects[1][2][3]. N

体外研究
(In Vitro)

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.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Nortriptyline 相关抗体:

Cell Viability Assay[3]

Cell Line: Human TCCSUP and mouse MBT-2 bladder cancer cells
Concentration: 6.25 μM, 12.5 μM, 25 μM, 50 μM and 100 μM
Incubation Time: 24, 48, or 72 h
Result: Exhibited cytotoxic effects on TCCSUP and MBT-2 cells.

Cell Cycle Analysis[3]

Cell Line: Human TCCSUP and mouse MBT-2 bladder cancer cells
Concentration: 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells)
Incubation Time: 24 h
Result: Caused cell cycle arrest in these bladder cancer cells.

Apoptosis Analysis[3]

Cell Line: Human TCCSUP and mouse MBT-2 bladder cancer cells
Concentration: 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells)
Incubation Time: 24 h
Result: Induced apoptosis in both TCCSUP and MBT-2 cells.

Western Blot Analysis[3]

Cell Line: Human TCCSUP and mouse MBT-2 bladder cancer cells
Concentration: 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells)
Incubation Time: 24 h
Result: 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.

体内研究
(In Vivo)

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]

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male C3H/HeN mice (25-30 g; 2-3 months of age) injected with MBT-2 cells[3]
Dosage: 10 or 20 mg/kg
Administration: Intraperitoneal injection; every day; for three weeks.
Result: Suppressed tumor growth in mice inoculated with MBT-2 cells.

Clinical Trial

分子量

263.38

Formula

C19H21N

CAS 号

72-69-5

性状

固体

颜色

White to off-white

结构分类
  • Alkaloids
  • Other Alkaloids
初始来源
  • 植物
  • 菊科
  • Centaurea bracteata Scop.
  • 植物
  • 唇形科
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

纯度 & 产品资料

纯度: 99.64%

Data Sheet (540 KB) SDS (252 KB)

COA (199 KB) HNMR (118 KB) RP-HPLC (187 KB)

产品使用指南 (1538 KB)

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.  [Content Brief]

    [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.  [Content Brief]

    [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.  [Content Brief]

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