产品
编 号:F482495
分子式:C17H19N3
分子量:265.35
产品类型
结构图
CAS No: 85650-52-8
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产品详情
生物活性:
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.
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.
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.