Mirtazapine (Org3770) 是一种有效的具有口服活性的去甲肾上腺素能和特异性血清素能抗抑郁剂 (NaSSA)。Mirtazapine 也是一种5-HT2、5-HT3，组胺 H1 受体 (histamine H1 receptor) 和 α2-肾上腺素受体 (α2-adrenoceptor) 拮抗剂，pKi值分别为 8.05、8.1、9.3 和 6.95。
| 生物活性 | Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a5-HT2,5-HT3,histamine H1 receptorandα2-adrenoceptorantagonist withpKivalues of 8.05, 8.1, 9.3 and 6.95, respectively[1][2]. |
| IC50& Target[2] | 5-HT3Receptor 8.1 (pKi) | 5-HT2Receptor 8.05 (pKi) | H1Receptor 9.3 (pKi) | α2-adrenergic receptor 6.95 (pKi) |
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体外研究
(In Vitro) | Mirtazapine can antagonize the adrenergic α2-autoreceptors and α2-heteroreceptors as well as block 5-HT2and 5-HT3receptors. Mirtazapine enhances the release of norepinephrine and 5-HT1A-mediated serotonergic transmission[1].
The cytochrome (CYP) P450 isoenzymes CYP1A2, CYP2D6, and CYP3A4 are mainly responsible for Mirtazapine's metabolism[1].
Mirtazapine (10 μM) significantly reduces activation-induced release of cytokine/chemokine mediators from human CD14+monocytes in vitro[3].
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体内研究
(In Vivo) | Mirtazapine (1-20 mg/kg; intraperitoneal injection; once; C57BL/6 mice) treatment strikingly and dose-dependently inhibits Con A-induced liver injury[3].
Mirtazapine treatment inhibits hepatic macrophage/monocyte activation, decreases hepatic macrophage/monocyte-derived pro-inflammatory cytokine (e.g., TNFα) and chemokine (e.g., CXCL1 and CXCL2) production, suppression of Con A-induced increases in the hepatic expression of the neutrophil relevant endothelial cell adhesion molecule ICAM-1, with the resultant significant reduction in neutrophil recruitment into the liver[3].
| Animal Model: | Male C57BL/6 mice (8-10 week old) treated with concanavalin A (Con A)[3] | | Dosage: | 1 mg/kg, 10 mg/kg, and 20 mg/kg | | Administration: | Intraperitoneal injection; once | | Result: | Strikingly and dose-dependently inhibited Con A-induced liver injury. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(188.43 mM;Need ultrasonic) H2O : 0.67 mg/mL(2.52 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.7686 mL | 18.8430 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 |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (9.42 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.42 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (9.42 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.42 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (9.42 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.42 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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