Mirtazapine

Từ đồng nghĩa: (±)-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.

Cấu trúc và tính chất hóa học

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.

Cơ chế tác dụng

• 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.

Tiêu chuẩn chất lượng

Cung ứng và Tài liệu

• Công suất: Monthly production capacity of 500 kg, scalable upon request.
• Thời gian thực hiện: 3-5 business days (stock items)
• Tài liệu hướng dẫn: COA, MSDS, TDS, DMF available upon request.
• Bao bì: 25 kg fiber drums with double polyethylene liners; smaller quantities available.

Yêu cầu báo giá

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