Agomelatine

同義語： N-[2-(7-Methoxynaphthalen-1-yl)ethyl]acetamide; Melatonin agonist; MT1/MT2 agonist; 5-HT2C antagonist; Agomelatine; S-20098; Valdoxan; Melitor

Agomelatine is a synthetic naphthalene derivative that stands out in the CNS space for its dual mechanism: it acts as a potent agonist at melatonin MT1 and MT2 receptors while simultaneously blocking serotonin 5-HT2C receptors. This combination is unusual—most antidepressants target monoamine transporters or single receptors—and it gives agomelatine a distinct pharmacological profile that resynchronizes circadian rhythms and enhances dopaminergic and noradrenergic transmission in the frontal cortex.

First approved in Europe in 2009 for major depressive episodes, agomelatine has since been studied for generalized anxiety disorder, seasonal affective disorder, and sleep regulation. The active pharmaceutical ingredient (API) is manufactured under cGMP conditions and is available in various polymorphic forms, with Form I being the most thermodynamically stable and commonly used in solid oral dosage forms. Our agomelatine is produced via a multi-step synthesis starting from 7-methoxy-1-tetralone, yielding high-purity material suitable for tablet formulation.

In the B2B segment, agomelatine is primarily supplied to generic drug manufacturers, research institutions, and specialty pharma companies developing reformulations or fixed-dose combinations. Its patent landscape has matured, opening opportunities for generic entry in multiple markets. The compound’s unique mechanism also attracts interest in chronobiology and neuropsychopharmacology research, where reliable, well-characterized API is essential.

化学構造と性質

Agomelatine features a 7-methoxynaphthalene core linked via an ethyl chain to an acetamide group. The methoxy substituent at the 7-position is critical for melatonin receptor affinity, while the acetamide side chain contributes to metabolic stability and oral bioavailability. The molecule is lipophilic (logP ≈ 2.5) and exhibits low aqueous solubility, which can be addressed through micronization or salt formation during formulation. It is optically inactive and exists as a single crystalline form under standard storage conditions.

作用機序

• Melatonin receptor agonism: Binds with high affinity to MT1 and MT2 receptors in the suprachiasmatic nucleus, resetting circadian phase and improving sleep architecture without sedative effects.
• 5-HT2C receptor antagonism: Blocks serotonin 2C receptors in the prefrontal cortex, leading to increased release of dopamine and norepinephrine—effects linked to improved mood and cognitive function.
• Circadian rhythm regulation: By targeting both melatonin and serotonin systems, agomelatine helps normalize disrupted biological rhythms often seen in depression.
• Neuroplasticity enhancement: Preclinical studies show increased BDNF expression and hippocampal neurogenesis, supporting its antidepressant efficacy.
• Anxiolytic effects: 5-HT2C blockade in limbic regions contributes to reduced anxiety, a common comorbidity in depressive disorders.

品質仕様

供給および書類

• 容量: 500 kg per month, scalable upon demand
• リードタイム: 3～5営業日（在庫品）
• ドキュメント: COA, MSDS, TDS, and regulatory support (DMF) provided upon request
• パッケージ: 25 kg fiber drum with double polyethylene bags, or as per customer requirements

見積依頼

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