Mianserin HCl |
Katalog-Nr.GC14726
One-Click Copy Product Info
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Mianserin HCl (Org GB 94) ist ein inverser Agonist des H1-Rezeptors und ein psychoaktiver Wirkstoff des tetrazyklischen Antidepressivums.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 21535-47-7
Sample solution is provided at 25 µL, 10mM.
Mianserin HCl is a tetracyclic compound, with a Ki value of 0.056 ± 0.012µM for 5-HT6R[1]. Mianserin HCl inhibits 5-HT-stimulated [Ca2+]i increase with an IC50 value of 16 ± 3.8nM and suppresses amplification by 5-HT of ADP-induced aggregation of canine platelets with an IC50 value of 3.18µM[2-3]. Mianserin HCl has been widely used to regulate dopamine levels in the prefrontal cortex of animals[4].
In vitro, Mianserin HCl treatment for 72h inhibited the proliferation of SW480 cells with an IC50 value of 37.5μM[5]. Treatment of Hep2 and Huh7 cells with 15μg/ml Mianserin HCl for 72 hours significantly inhibited cell viability and induced cell apoptosis[6].
In vivo, Mianserin HCl treatment via daily intraperitoneal injection at a dose of 2mg/kg for 3 weeks blocked both 5-HT-2 and 5-HT-1A receptors in a rat model of depression[7]. Intra-articular injection of 50μM Mianserin HCl (50μl) into both knees once a week for 8 weeks prevented cartilage degeneration in a rat model of osteoarthritis and inhibited Wnt/β-catenin signaling in articular chondrocytes[8].
References:
[1] Więckowski K, Szałaj N, Gryzło B, et al. Serotonin 5-HT6 receptor ligands and butyrylcholinesterase inhibitors displaying antioxidant activity—design, synthesis and biological evaluation of multifunctional agents against Alzheimer’s disease[J]. International Journal of Molecular Sciences, 2022, 23(16): 9443.
[2] Ohsuka N, Mashiko H, Kaneko M, et al. Effects of Antidepressants and antipsychotics on the 5HT2 receptor-mediated signal transducing system in human platelets[J]. Psychopharmacology, 1995, 121(4): 428-432.
[3] Bush L R. Effects of the serotonin antagonists, cyproheptadine, ketanserin and Mianserin HCl, on cyclic flow reductions in stenosed canine coronary arteries[J]. The Journal of pharmacology and experimental therapeutics, 1987, 240(2): 674-682.
[4] Tanda G, Bassareo V, Chiara D. Mianserin HCl markedly and selectively increases extracellular dopamine in the prefrontal cortex as compared to the nucleus accumbens of the rat[J]. Psychopharmacology, 1996, 123(2): 127-130.
[5] Duan Z, Zhou Z, Lu F, et al. Antitumor activity of Mianserin HCl (a tetracyclic antidepressant) primarily driven by the inhibition of SLC1A5-mediated glutamine transport[J]. Investigational New Drugs, 2022, 40(5): 977-989.
[6] Huang Y H, Yeh C T. Anticancer effects of antidepressants in hepatocellular carcinoma cells[J]. Anticancer research, 2023, 43(3): 1201-1206.
[7] Jotaro A, Kounosuke T, Yuuko M, et al. Effects of chronic Mianserin HCl administration on serotonin metabolism and receptors in the 5-hydroxytryptophan depression model[J]. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 1994, 18(1): 165-179.
[8] Okura T, Ohkawara B, Takegami Y, et al. Mianserin HCl suppresses R-spondin 2-induced activation of Wnt/β-catenin signaling in chondrocytes and prevents cartilage degradation in a rat model of osteoarthritis[J]. Scientific Reports, 2019, 9(1): 2808.
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were grown in Dulbecco’s modified Eagle’s medium (DMEM) supplemented with 10% fetal bovine serum in a humidified 37°C incubator with 5% CO2. Cells were cultured in 96-well microplates for 24h. Then, several different concentrations (5, 15, 25, 35, 45, 55, 65, 75, and 85μg/ml) of Mianserin HCl were prepared and applied to the cells. After 72h of incubation, the media containing the MTT solution were provided. Four hours later, the solubilization solution was added for overnight incubation. The cell proliferation index was measured by optical density at 570nm. |
Reaction Conditions | 5, 15, 25, 35, 45, 55, 65, 75, and 85μg/ml; 72h |
Applications | Mianserin HCl treatment significantly inhibited the viability of HepG2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male BALB/c nude mice |
Preparation Method | Male BALB/c nude mice (4-6 weeks old) were maintained under standard conditions. To establish a colorectal tumor model, approximately 5×106 SW480 cells were collected, mixed with Matrigel at a 1:1 volume ratio, and injected into the lower back of each mouse. When the tumor volume reached 100-150mm3, the tumor-bearing mice were randomly divided into 2 groups (N=6). Treatment regimens (by intraperitoneal injection every 3 days) were as follows: (A) control group, 10ml/kg vehicle (5% PEG400:95% saline) and (B) Mianserin HCl group (30mg/kg Mianserin HCl treatment). A dose of Mianserin HCl of 30mg/kg was chosen to be given every three days for 20 days. The body weight of the mice was recorded, and the tumor size was measured every 3 days with a digital caliper. |
Dosage form | 30mg/kg every three days for 20 days; i.p. |
Applications | Mianserin HCl treatment inhibited SW480 tumor growth without affecting body weight in SW480 xenograft nude mice. |
References: | |
| Cas No. | 21535-47-7 | SDF | |
| Chemical Name | 2-methyl-1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine hydrochloride | ||
| Canonical SMILES | CN1CC2C3=C(C=CC=C3)CC4=C(C=CC=C4)N2CC1.Cl | ||
| Formula | C18H20N2.HCl | M.Wt | 300.83 |
| Löslichkeit | ≥ 15.0415mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3241 mL | 16.6207 mL | 33.2414 mL |
| 5 mM | 664.8 μL | 3.3241 mL | 6.6483 mL |
| 10 mM | 332.4 μL | 1.6621 mL | 3.3241 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
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Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)