イストラデフィリン 化学特性,用途語,生産方法
外観
白色～うすい黄緑色, 結晶～粉末
溶解性
ジメチルスルホキシドに可溶
用途
アデノシンA2A 受容体拮抗剤
です。GABA 神経の過剰興奮を抑制します。
効能
パーキンソン病治療薬, アデノシンA2A受容体拮抗薬
商品名
ノウリアスト (協和発酵キリン)
説明
In March 2013, istradefylline (also known as KW-6002) was approved in Japan for adjunctive treatment of Parkinson’s disease (PD). Istradefylline acts by antagonism of the adenosine A
2A receptor, which is colocalized with dopamine D
2 receptors in the striatum, to enhance dopamine D
2-dependent signaling. Istradefylline is a light-sensitive compound and has been evaluated in vitro under low-light conditions to prevent isomerization of the (E)-styryl group and decomposition. Istradefylline has a Ki of 2.2 nM for the rat adenosine A
2A receptor and an ED
50 of 0.03 mg/kg, po, in reversal of haloperidol-induced catalepsy in mice. Further characterization showed istradefylline to have a Ki of 12 nM for the human adenosine A
2A receptor, to be highly selective, and to be a functional competitive antagonist. Istradefylline has activity alone and in combination with levo-dopa in preclinical animal models of PD. The synthesis of istradefylline was accomplished by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide-mediated coupling of 5,6-diamino-1,3-diethyluracil with 3,4-dimethoxycinnamic acid, followed by cyclization upon treatment with aqueous NaOH, and selective methylation (MeI, K
2CO
3, and DMF).
使用
Treatment of
Parkinson’s disease (adenosine A 2A receptor antagonist).
イストラデフィリン 上流と下流の製品情報
原材料
準備製品