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 |
|
注意: |
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