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Mirtazapine

CAS No. : 85650-52-8

MCE 国际站：Mirtazapine

产品活性：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，pK_i 值分别为 8.05、8.1、9.3 和 6.95。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：5-HT Receptor  |  Histamine Receptor  |  Adrenergic Receptor

In Vitro: 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.

In Vivo: 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.

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