4-AP
関連概念 : 化学

[4AP: 4-aminopyridine :dalfampridine]

H2NC5H4N。

   

ピリジンの3つのisomeric aminesのうちの一。
Kチャネルの阻害剤(Grissmer et al.,1994)。

【特徴】

 ◆製造
  decarbonylation of pyridine-4-carboxamide
    using sodium hypochlorite via the Hofmann rearrangement
  The pyridine carboxamide is generated from
    the corresponding nitrile, which in turn is obtained
    from ammoxidation of 4-methylpyridine
 ◆Applications
  ・Kチャネルの阻害剤
    Kv1 (Shaker, KCNA) familyに比較的選択性強い(1mM程度まで)
  ・potent calcium channel(beta subunit) activator
    (J Biol Chem. 2009 Dec 25;284(52):36453-61)
 ◆臨床
  ・Lambert-Eaton myasthenic syndrome
  ・multiple sclerosis
    improve visual function and motor skills
    relieve fatigue in patients with Multiple Sclerosis (MS)
     特にchronic progressive form of MSに有効
  ・副作用
    dizziness, nervousness and nausea,
    and the incidence of adverse effects(<5%)
    過剰摂取でparesthesias, seizures, and atrial fibrillation

2011/05/31 masashi tanaka

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