イミダフェナシン 化学特性,用途語,生産方法
効能
過活動膀胱用薬, ムスカリン受容体拮抗薬
商品名
ウリトス (杏林製薬); ステーブラ (小野薬品工業)
説明
Imidafenacin, an M3/M1 muscarinic receptor antagonist, was introduced in
Japan for the oral treatment of OAB. The majority of OAB symptoms are
thought to result from overactivity of the detrusor muscle, which is primarily
mediated by acetylcholine-induced stimulation of muscarinic M3 receptors in the
bladder. Previously marketed muscarinic antagonists for OAB include propiverine,
tolterodine, oxybutynin, trospium, darifenacin, and solifenacin. In vitro,
imidafenacin is equally active against M1 and M3 receptors (K
b＝0.32 and
0.55nM, respectively), and approximately 10-fold less active against M2 receptors
(K
b＝4.13nM).
Imidafenacin is chemically synthesized in three steps starting with alkylation of diphenylacetonitrile with dibromoethane, followed by condensation with 2-methylimidazole, and hydrolysis of the cyano group to a carboxamide group with 70% sulfuric acid.
化学的特性
White Solid
使用
Imidafenacin-d10 is deutirium labelled imidafenacin which is a novel therapeutic agent for overactive bladder with antimuscarinic activity, on mediator release from urothelium and detrusor overactivity induced by cerebral infarction.
副作用
Like all medicines, imidafenacin can cause side effects, but not everybody will experience them. This drug can cause sleepiness, blurred vision, stomach upset, constipation, and increased triglyceride levels.
イミダフェナシン 上流と下流の製品情報
原材料
準備製品