ウラピジル塩酸塩 化学特性,用途語,生産方法
効能
血圧降下薬, α1アドレナリン受容体拮抗薬
説明
Urapidil is an antagonist of α
1-adrenergic receptors (α
1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT
1A. It selectively binds to α
1- over α
2-ARs (IC
50s = 0.74 and 42 μM, respectively) and to 5-HT
1A over 5-HT
1B and 5-HT
2 receptors (IC
50s = 0.4, 20.4, and >10 μM, respectively) in rat cortex. Urapidil inhibits cAMP accumulation induced by forskolin in calf hippocampus as a functional model for 5-HT
1A receptors (EC
50 = 390 nM). It is also a β
1-AR antagonist that inhibits the positive chronotropic response induced by isoproterenol in isolated rat atria (pA
2 = 6.05). Urapidil (1 μmol/kg, i.v.) lowers mean arterial pressure (MAP) in anesthetized cats, an effect that is reduced by central administration of the 5-HT
1A receptor antagonist spiroxatrine.
化学的特性
White to Off-White Crystalline Powder
使用
a1-Adrenergic antagonist; derivative of Uracil. Antihypertensive
生物活性
α 1 -adrenoceptor antagonist and 5-HT 1A receptor agonist (pIC 50 values are 6.13 and 6.4 respectively). Clinically used hypotensive agent.
副作用
Side effects that may occur during treatment with uradil antihypertension include dizziness, fatigue, nausea, and light-headedness effects. The increases in systolic blood pressure heart rate caused by three progressive work loads bicycle exercise were not affected during urapidil, A slight reduction in forced expiratory volume was observed in some patients during treatment with beta-blocker. There was no case orthostatic hypotension during urapidil administration, despite its alpha1-blocking action. Side-effects were rare negligible
[1].
ウラピジル塩酸塩 上流と下流の製品情報
原材料
準備製品