Mianserin

目录号: GC15518纯度: >98%同义词: 米安色林; Mianserine

Mianserin是一种四环类化合物，对5-HT6受体的K_i值为0.056 ± 0.012µM。

Cas No.: 24219-97-4

规格	价格	库存	数量
5mg	¥321.00	现货	1
10mg	¥459.00	现货	1
25mg	¥788.00	现货	1
50mg	¥1,262.00	现货	1
100mg	¥2,027.00	现货	1

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610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
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产品描述 Description

Mianserin is a tetracyclic compound, with a K_i 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K_i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]。

实验参考方法 Experimental Reference Method

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: [1] Huang Y H, Yeh C T. Anticancer effects of antidepressants in hepatocellular carcinoma cells[J]. Anticancer research, 2023, 43(3): 1201-1206. [2] 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.

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

24219-97-4

同义词

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

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 g/mol

溶解性

Soluble in DMSO; >16 mg/mL in DMSO; >50 mg/mL in Methanol with ultrasonic; >10 mg/mL in EtOH with ultrasonic

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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