Mirtazapine

SKU: orb1223846

Description

Mirtazapine is an antidepressant introduced by Organon International in 1996 used for the treatment of moderate to severe depression. Mirtazapine has a tetracyclic chemical structure and is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). It is the only tetracyclic antidepressant that has been approved by the Food and Drug Administration to treat depression. (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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 85650-52-8
• MW: 265.35
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₉N₃
• SMILES: CN1CCN2C(C3=CC=CC=C3CC4=C2N=CC=C4)C1
• Target: 5-HT Receptor
• Solubility: Ethanol: 53 mg/mL (199.73 mM); DMSO: 53 mg/mL (199.73 mM)

Bioactivity

• 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. 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

6-Azamianserin | ORG 3770

Quick Database Links

Gene Symbol

5-HT Receptor