Mianserin HCl
(Synonyms: 盐酸米安色林; Org GB 94) 目录号 : GC14726
Mianserin HCl是一种四环类化合物，对5-HT6受体的Ki值为0.056 ± 0.012µM。
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.
Mianserin HCl是一种四环类化合物，对5-HT6受体的Ki值为0.056 ± 0.012µM[1]。Mianserin HCl可抑制5-HT刺激的细胞内钙离子（[Ca2+]i）增加（IC50=16 ± 3.8nM），并能抑制由5-HT扩增的ADP诱导的犬血小板聚集（IC50=3.18µM）[2-3]。Mianserin HCl已广泛应用于动物模型中调节前额叶皮质多巴胺水平[4]。
在体外，Mianserin HCl处理72小时可抑制SW480细胞增殖，IC50值为37.5μM[5]。15μg/ml的Mianserin HCl处理Hep2和Huh7细胞72小时能显著抑制细胞活力并诱导凋亡[6]。
在体内，每日以2mg/kg剂量腹腔注射Mianserin HCl持续3周可阻断抑郁模型大鼠额叶皮质5-HT-2和5-HT-1A受体[7]。骨关节炎大鼠模型每周双膝关节腔内注射50μM的Mianserin HCl（50μl）持续8周能预防软骨退化并抑制关节软骨中Wnt/β-catenin信号通路[8]。
| 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 | |
| 别名 | 盐酸米安色林; Org GB 94 | ||
| 化学名 | 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 | ||
| 分子式 | C18H20N2.HCl | 分子量 | 300.83 |
| 溶解度 | ≥ 15.0415mg/mL in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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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 |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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Quality Control & SDS
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- Purity: >99.50%
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