S81014 |
Mirtazapine |
源叶(MedMol) | 99% |
- 产品描述: Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively
- 靶点: 5-HT3 Receptor:8.1 (pKi);5-HT2 Receptor:8.05 (pKi);H1 Receptor:9.3 (pKi);α2-adrenergic receptor:6.95 (pKi);DopamineReceptor; 5-HTReceptor; OpioidReceptor; AdrenergicReceptor; HistamineReceptor
- 体外研究:
Mirtazapine can antagonize the adrenergic α2-autoreceptors and α2-heteroreceptors as well as block 5-HT2 and 5-HT3 receptors. Mirtazapine enhances the release of norepinephrine and 5-HT1A-mediated serotonergic transmission. The cytochrome (CYP) P450 isoenzymes CYP1A2, CYP2D6, and CYP3A4 are mainly responsible for Mirtazapine's metabolism. Mirtazapine (10 μM) significantly reduces activation-induced release of cytokine/chemokine mediators from human CD14+ monocytes in vitro
- 体内研究:
Mirtazapine (1-20 mg/kg; intraperitoneal injection; once; C57BL/6 mice) treatment strikingly and dose-dependently inhibits Con A-induced liver injury. 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. Animal Model: Male C57BL/6 mice (8-10 week old) treated with concanavalin A (Con A) 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.
- 参考文献:
1. S A Anttila, et al. A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. Fall 2001;7(3):249-64. 2. T H de Boer, et al. Neurochemical and autonomic pharmacological profiles of the 6-aza-analogue of mianserin, Org 3770 and its enantiomers. Neuropharmacology. 1988 Apr;27(4):399-408. 3. Wagdi Almishri, et al. The Antidepressant Mirtazapine Inhibits Hepatic Innate Immune Networks to Attenuate Immune-Mediated Liver Injury in Mice. Front Immunol. 2019 Apr 12;10:803.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.769 ml 18.843 ml 37.686 ml 5 mM 0.754 ml 3.769 ml 7.537 ml 10 mM 0.377 ml 1.884 ml 3.769 ml 50 mM 0.075 ml 0.377 ml 0.754 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)