Mirtazapine

同義語： (±)-1,2,3,4,10,14b-Hexahydro-2-methylpyrazino[2,1-a]pyrido[2,3-c][2]benzazepine, Mirtazapine, Remeron, Zispin, Norset, Avanza, Mirtazapine API

Mirtazapine is a tetracyclic piperazino-azepine antidepressant that acts as an antagonist at central presynaptic α2-adrenergic autoreceptors and heteroreceptors. By blocking these receptors, it increases noradrenergic and serotonergic neurotransmission—a mechanism distinct from SSRIs and SNRIs. The molecule also shows potent antagonism at 5-HT2 and 5-HT3 receptors, plus significant antihistamine (H1) activity.

First approved in the mid-1990s, mirtazapine is now a standard treatment for major depressive disorder, often chosen when insomnia and appetite loss are prominent. It is available as immediate-release tablets and orally disintegrating tablets. The active pharmaceutical ingredient (API) is manufactured under cGMP and supplied in various particle sizes for solid dosage formulation.

化学構造と性質

Mirtazapine belongs to the chemical class of piperazino-azepines. Its structure features a fused tetracyclic ring system with a methylpiperazine moiety. The compound is a white to off-white crystalline powder, practically insoluble in water, but freely soluble in methanol and slightly soluble in ethanol. It exhibits no chiral center and is used as the racemate. The molecular formula is C17H19N3, and its molecular weight is 265.35 g/mol.

作用機序

• α2-adrenergic antagonism: Blocks presynaptic α2 autoreceptors and heteroreceptors, increasing release of norepinephrine and serotonin.
• 5-HT2 receptor antagonism: Reduces serotonin-related side effects like insomnia and sexual dysfunction; contributes to anxiolytic effects.
• 5-HT3 receptor antagonism: May reduce nausea and improve sleep architecture.
• H1 histamine antagonism: Produces sedative effects, often beneficial for depressed patients with insomnia.

品質仕様

供給および書類

• 容量: Monthly production capacity of 500 kg, scalable upon request.
• リードタイム: 3～5営業日（在庫品）
• ドキュメント: COA, MSDS, TDS, DMF available upon request.
• パッケージ: 25 kg fiber drums with double polyethylene liners; smaller quantities available.

見積依頼

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