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Nortriptyline, an active metabolite of amitriptyline, is a second-generation antidepressant developed by Lilly for use in major depression, childhood nocturnal enuresis, dysthymia, and atypical depressions. It is a non-selective monoamine reuptake inhibitor.
| ln Vitro |
CYP2C19 helps amitriptyline convert to nortriptyline, which is its active metabolite. More so than serotonin, nortriptyline inhibits nortriptyline refeeding [1]. In a concentration- and time-stable manner, nortriptyline (6.25-100 μM; 24-72 hours) dramatically lowers both bladder MBT-2 bladder viability and TCCSUP [3]. In TCCSUP and MBT-2 cells, nortriptyline (12.55-100 μM; 24 hours) stimulates cell cycle signaling and cell bladder [3]. These inner and outer vaginal cells are induced by TCCSUP and MBT-2 cells at concentrations of 25 μM, 50 μM, or 100 μM (TCCSUP; 12.55-100 μM; 24 hours). In these bladder cancer cells, exposure to 12.5 μM, 25 μM, or 50 μM (MBT-2 cells) for a whole day caused cell cycle arrest. TCCSUP and MBT-2 cells undergo apoptosis when exposed to 25 μM, 50 μM, or 100 μM (TCCSUP); 12.5 μM, 25 μM, or 50 μM (MBT-2 cells). This apoptotic response lasts for 24 hours and increases the levels of Fas, FasL, FADD, Bax, Bak, and caspase-3, caspase-8, caspase-9, and poly(ADP-ribose) polymerase. decreases the expression of survivin, X-linked apoptosis protein inhibitor, BH3 interaction domain death agonist, Bcl-2, and Bcl-xL.
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| ln Vivo |
In MBT-2 cells, nortriptyline (10–20 mg/kg) administered intraperitoneally once a day for three weeks reduces the formation of bladder tumors [3].
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| Cell Assay |
Cell Viability Assay[3]
Cell Types: Human TCCSUP and Mouse MBT-2 Bladder Cancer Cells Tested Concentrations: 6.25 μM, 12.5 μM, 25 μM, 50 μM and 100 μM Incubation Duration: 24, 48 or 72 hrs (hours) Experimental Results: Cells exhibit Toxic effects on TCCSUP and MBT-2 cells. Cell cycle analysis[3] Cell Types: human TCCSUP and mouse MBT-2 Bladder cancer cell Tested Concentrations: 25 μM, 50 μM or 100 μM (TCCSUP); 12.5 μM, 25 μM or 50 μM (MBT-2 cells) Incubation Duration: 24 hour Experimental Results: Caused cell cycle arrest in these bladder cancer cells. Apoptosis analysis[3] Cell Types: human TCCSUP and mouse MBT-2 Bladder cancer cells Tested Concentrations: 25 μM, 50 μM or 100 μM (TCCSUP); 12.5 μM, 25 μM or 50 μM (MBT-2 cells) Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis in TCCSUP and MBT-2 cells. Western Blot Analysis[3] Cell Types: human TCCSUP and mouse MBT-2 Bladder cancer cells Tested Concentrations: 25 μM, 50 μM or 100 μM (TCCSUP); 12.5 μM, 25 μM or 50 μM (MBT-2 cells) Incubation Duration: 24 hrs (hours) Experimental Results: Increased expression of Fas, Fa |
| Animal Protocol |
Animal/Disease Models: Adult male C3H/HeN mice (25-30 g; 2-3 months old) were injected with MBT-2 cells [3]
Doses: 10 or 20 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; three Week. Experimental Results: Tumor growth was inhibited in mice vaccinated with MBT-2 cells. |
| References |
[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. |
| Molecular Formula |
C19H21N
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|---|---|
| Molecular Weight |
263.37674
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| CAS # |
72-69-5
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| Related CAS # |
Nortriptyline hydrochloride;894-71-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
CNCC/C=C1\C2=CC=CC=C2CCC2=CC=CC=C\12
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7968 mL | 18.9840 mL | 37.9680 mL | |
| 5 mM | 0.7594 mL | 3.7968 mL | 7.5936 mL | |
| 10 mM | 0.3797 mL | 1.8984 mL | 3.7968 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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