マレイン酸エナラプリル 化学特性,用途語,生産方法
外観
白色～ほとんど白色, 結晶性粉末～粉末
溶解性
メタノールには溶けやすく、エタノールにやや溶けやすく、水にやや溶けにくく、アセトニトリルに溶けにくく、エーテルに極めて溶けにくい。
用途
アンジオテンシン変換酵素 （ACE-1）阻害剤です。アンジオテンシン変 換酵素を阻害し、アンジオテンシンⅡ生成抑 制作用を示します。
用途
アンジオテンシン変換酵素
（ACE）阻害剤です。アンジオテンシン変換
酵素を阻害し、アンジオテンシンⅡ生成抑制
作用を示します。
用途
高血圧の研究。
効能
血圧降下薬, 血管拡張薬, アンジオテンシン変換酵素(ACE)阻害薬
商品名
エナラプリルマレイン酸塩 (キョーリンリメディオ); レニベース (MSD)
説明
Enalapril maleate is the second angiotensin converting enzyme inhibitor to reach
the marketplace. Like captopril, the first entry in this area, enalapril is useful in
the treatment of hypertension and congestive heart failure. It has a longer effective
half-life than captopril, allowing once or twice-daily dosing, and appears to have a
somewhat lower incidence of side effects.
化学的特性
White to Off-White Crystalline Powder
使用
Enalapril maleate salt is used as a long-acting ACE inhibitor and antihypertensive, used to study diabetic angiopathy in diabetic rats and inhibition of ACE in hog plasma (I50=1.2nM). ACE inhibitors disturb the enin-angiotensin- aldosterone system. Additional ACE inhibitors include: Enalapril, Enalaprilat dihydrate, Enalaprilat, and Enalapril-d5 Maleate Salt, among others.
定義
ChEBI: The maleic acid salt of enalapril. It contains one molecule of maleic acid for each molecule of enalapril. Following oral administration, the ethyl ester group of enalapril is hydrolysed to afford the corresponding carboxylic acid, enalaprilat, an angioten
in-converting enzyme (ACE) inhibitor. Enalapril is thus a prodrug for enalaprilat (which, unlike enalapril, is not absorbed by mouth), and its maleate is used in the treatment of hypertension and heart failure, for reduction of proteinuria and renal diseas
in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients.
一般的な説明
Enalapril maleate, 1-[N[(S)-1-carboxy-3-phenylpropyl]-L-alanyl]-L-proline 1 -ethyl estermaleate (Vasotec), is a long-acting ACE inhibitor. It requiresactivation by hydrolysis of its ethyl ester to form thediacid enalaprilat. Enalapril is devoid of the side effects ofrash and loss of taste seen with captopril. These side effectsare similar to those of the mercapto-containing drugpenicillamine. The absence of the thiol group in enalaprilmaleate may free it from these side effects. The half-life is11 hours.
マレイン酸エナラプリル 上流と下流の製品情報
原材料
準備製品