Mianserin
(Synonyms: 米安色林; Mianserine) 目录号 : GC15518
Mianserin是一种四环类化合物，对5-HT6受体的Ki值为0.056 ± 0.012µM。
Cas No.:24219-97-4
Sample solution is provided at 25 µL, 10mM.
Mianserin is a tetracyclic compound, with a Ki value of 0.056 ± 0.012µM for 5-HT6R[1]. Mianserin 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 has been widely used to regulate dopamine levels in the prefrontal cortex of animals[4].
In vitro, Mianserin 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 for 72 hours significantly inhibited cell viability and induced cell apoptosis[6].
In vivo, Mianserin 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 (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, 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 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 (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 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 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是一种四环类化合物，对5-HT6受体的Ki值为0.056 ± 0.012µM[1]。Mianserin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处理72小时可抑制SW480细胞增殖，IC50值为37.5μM[5]。15μg/ml的Mianserin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（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 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 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 group (30mg/kg Mianserin treatment). A dose of Mianserin 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 treatment inhibited SW480 tumor growth without affecting body weight in SW480 xenograft nude mice. |
References: | |
| Cas No. | 24219-97-4 | SDF | |
| 别名 | 米安色林; Mianserine | ||
| 化学名 | (R)-3-methyl-1,2,3,4,4a,9-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine | ||
| Canonical SMILES | [H]C1(C2=C([H])C([H])=C([H])C([H])=C2C([H])([H])C3=C([H])C([H])=C([H])C([H])=C43)N4C([H])([H])C([H])([H])N(C([H])([H])[H])C1([H])[H] | ||
| 分子式 | C18H20N2 | 分子量 | 264.36 |
| 溶解度 | Soluble in DMSO; >16 mg/mL in DMSO; >50 mg/mL in Methanol with ultrasonic; >10 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7827 mL | 18.9136 mL | 37.8272 mL |
| 5 mM | 756.5 μL | 3.7827 mL | 7.5654 mL |
| 10 mM | 378.3 μL | 1.8914 mL | 3.7827 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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