Mirtazapine
(Synonyms: 米氮平) 目录号 : GC11447
Mirtazapine是一种去甲肾上腺素能和特异性血清素抗抑郁药（NaSSA），可抑制5-HT2A、5-HT2B、5-HT2C和5-HT3受体，pKi值分别为8.2、6.7、7.9和8.1。
Cas No.:85650-52-8
Sample solution is provided at 25 µL, 10mM.
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Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) that inhibits 5‐HT2A, 5‐HT2B, 5‐HT2C, and 5‐HT3 receptors, with pKi values of 8.2, 6.7, 7.9 and 8.1, respectively. Mirtazapine can inhibit the presynaptic alpha-2-adrenergic receptors, and induce the release of norepinephrine and serotonin[2].
In vitro, Mirtazapine treatment at 10μM for 24h in SAS-H1 cells increased Lin-7C/β-catenin pathway activity, resulting in a decrease in cell migration[3]. Mirtazapine treatment at 10μM for 24h resulted in a rapid decrease in mouse hepatic B cell numbers and altered hepatic B1a and B2 subgroup profiles, increased CXCL10 levels, and upregulated CXCR3 expression by intrahepatic B cells[4]. Pretreatment of SH-SY5Y cells with 2μM Mirtazapine for 24 hours inhibited H2O2-induced cell death, decreased p53 mRNA expression, and increased Bcl-2/Bax protein ratio[5].
In vivo, Mirtazapine (16mg/kg) administered intraperitoneally to mouse models of Parkinson’s disease once daily for 8 days significantly reduced the loss of dopaminergic neurons on the injured side and promoted astrocyte proliferation and MT-1/2 up-regulation in the striatum[6]. Daily oral administration of 10mg/kg Mirtazapine in CT26/luc colon carcinoma-bearing mouse model for 67 days resulted in a significant reduction in tumor volume[7].
References:
[1] Anttila S A K, Leinonen E V J. A review of the pharmacological and clinical profile of mirtazapine[J]. CNS drug reviews, 2001, 7(3): 249-264.
[2] Park Y S, Oh H, Sung K W. Atypical antidepressant mirtazapine inhibits 5-hydroxytryptamine3 receptor currents in NCB-20 cells[J]. Journal of Pharmacological Sciences, 2023, 151(2): 63-71.
[3] Uzawa K, Kasamatsu A, Shimizu T, et al. Suppression of metastasis by mirtazapine via restoration of the Lin-7C/β-catenin pathway in human cancer cells[J]. Scientific reports, 2014, 4(1): 5433.
[4] Almishri W, Davis R P, Shaheen A A, et al. The antidepressant mirtazapine rapidly shifts hepatic b cell populations and functional cytokine signatures in the mouse[J]. Frontiers in Immunology, 2021, 12: 622537.
[5] Lieberknecht V, Engel D, Rodrigues A L S, et al. Neuroprotective effects of mirtazapine and imipramine and their effect in pro-and anti-apoptotic gene expression in human neuroblastoma cells[J]. Pharmacological Reports, 2020, 72(3): 563-570.
[6] Kikuoka R, Miyazaki I, Kubota N, et al. Mirtazapine exerts astrocyte-mediated dopaminergic neuroprotection[J]. Scientific reports, 2020, 10(1): 20698.
[7] Fang C K, Chen H W, Chiang I T, et al. Mirtazapine inhibits tumor growth via immune response and serotonergic system[J]. PloS one, 2012, 7(7): e38886.
Mirtazapine是一种去甲肾上腺素能和特异性血清素抗抑郁药（NaSSA），可抑制5-HT2A、5-HT2B、5-HT2C和5-HT3受体，pKi值分别为8.2、6.7、7.9和8.1[1]。Mirtazapine通过抑制突触前alpha2-肾上腺素能受体，促进去甲肾上腺素和血清素的释放[2]。
在体外，10μM的Mirtazapine处理SAS-H1细胞24小时可增强Lin-7C/β-catenin通路活性，抑制细胞迁移[3]。10μM的Mirtazapine处理小鼠肝脏B细胞24小时会快速减少B细胞数量，改变肝脏B1a和B2亚群分布，提高CXCL10水平并上调肝内B细胞的CXCR3表达[4]。2μM的Mirtazapine预处理SH-SY5Y细胞24小时能抑制H2O2诱导的细胞死亡，降低p53 mRNA表达，并提高Bcl-2/Bax蛋白比例[5]。
在体内，帕金森病模型小鼠每日腹腔注射Mirtazapine（16mg/kg）连续8天，可显著减少损伤侧多巴胺能神经元丢失，并促进纹状体星形胶质细胞增殖及MT-1/2上调[6]。在携带 CT26/luc 结肠癌的实验小鼠模型中，每日口服给予10mg/kg剂量的Mirtazapine，持续 67 天，导致肿瘤体积显著减小[7]。
| Cell experiment [1]: | |
Cell lines | Human SH-SY5Y neuroblastoma cells |
Preparation Method | Human SH-SY5Y neuroblastoma cells were maintained at 37 °C in 95% air and 5% CO2. Cells grew in DMEM (10% of FBS and 1% of a mixture of penicillin at 1000U/mL)/streptomycin at 10mg/mL). SH-SY5Y cells were cultured in a monolayer and subcultured when the cells reached a confluence of 75–80%. Before each experiment, trypsin was added to the cells (0.25% trypsin-EDTA). Next, cells were centrifuged (1100rpm for 5min) and seeded at a density of 4.2 × 104 cells/cm2 in 96-well plates for the viability assays or in 48-well plates for the comet assays. Cells were used with a maximum passage number of 15. Mirtazapine was dissolved in DMSO (0.1% in cell culture medium), the concentrations tested in the cells ranged between 0.01, 0.1, 1, 10, and 20µM. H2O2 (10µM-300µM) was dissolved in sterilized water (0.1% in cell culture medium). A stock solution of Methyl Methanesulfonate (MMS) was prepared in sterilized water and further diluted in cell culture medium to a working concentration of 0.5mM. For Mirtazapine and Mirtazapine/H2O2 combinations, vehicles were composed of 0.1% DMSO in cell culture medium. For H2O2, vehicle was composed of 0.1% of sterilized water in cell culture medium. All the treatments were tested in a period of 48h after the cell attachment to the plates except MMS, which was used as a positive control for comet assays, being in contact with the cells for 1h. |
Reaction Conditions | 0.01, 0.1, 1, 10, and 20µM; 48h |
Applications | Mirtazapine significantly prevented the decline in cell viability caused by H2O2 in SH-SY5Y neuroblastoma cells. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | CT26/luc cells (2×106 cells/200µL) suspended in the serum-free RPMI medium were transplanted subcutaneously into the dorsal region of the right thighs of the BALB/c mice. 10mg/kg/day Mirtazapine dissolved in 0.9% sodium chloride and 0.5% ethanol was administered to mice by gavage daily till mice expired or terminated on day 67 post tumor inoculation. Survival rate and interval were assayed (n = 10 per group). Tumor growth was monitored using a digital caliper twice a week. The tumor volume was calculated according to the formula: 0.523× length × width × thickness. |
Dosage form | 10mg/kg/day for 67 days; p.o. |
Applications | Mirtazapine inhibited tumor growth and increased the survival rate of tumor-bearing mice during the 22-47 days after tumor inoculation. |
References: | |
| Cas No. | 85650-52-8 | SDF | |
| 别名 | 米氮平 | ||
| 化学名 | 2-methyl-1,2,3,4,10,14b-hexahydrobenzo[c]pyrazino[1,2-a]pyrido[3,2-f]azepine | ||
| Canonical SMILES | [H]C1(C2=C([H])C([H])=C([H])C([H])=C2C([H])([H])C3=C4N=C([H])C([H])=C3[H])N4C([H])([H])C([H])([H])N(C([H])([H])[H])C1([H])[H] | ||
| 分子式 | C17H19N3 | 分子量 | 265.35 |
| 溶解度 | ≥ 11.9mg/mL in DMSO | 储存条件 | Store at 2-8°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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7686 mL | 18.843 mL | 37.6861 mL |
| 5 mM | 0.7537 mL | 3.7686 mL | 7.5372 mL |
| 10 mM | 0.3769 mL | 1.8843 mL | 3.7686 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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- Purity: >99.50%
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