イルベサルタン 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
用途
アンジオテンシンⅡ受容体拮 抗剤です。アンジオテンシンⅡ受容体タイプ Ⅰ（ AT1）受容体に作用を示します。
用途
アンジオテンシンⅡ受容体拮
抗剤です。アンジオテンシンⅡ受容体タイプ
Ⅰ（AT1）受容体に作用を示します。
効能
血圧降下薬, アンジオテンシンII受容体拮抗薬
商品名
アバプロ (大日本住友製薬); イルベタン (シオノギファーマ)
説明
Avapro was launched in Germany, the UK and the US for hypertension. It
can be prepared in six steps starting with cyclopentanone or in three steps from 1-
aminocyclopentanecarboxylic acid ethyl ester and pentanimidic ethyl ester. Avapro is
an angiotensin Ⅱ receptor antagonist that is non-competitive and selective for AT,
subtypes and has no AT
2 activity at postsynaptic receptors compared to presynatpic. It
has no affinity for various non angiotensin Ⅱ receptor types in binding, no interaction
with calcium channels or antiports, and no affinity for α
1- and α
2--adrenoreceptors,
serotonergic receptors, muscarinic m
1 and m
2 or other receptors. It is as potent as
saralasin but with no agonist activity and is 10 times more potent than DuP753 in rats.
It is similar in efficacy to enalapril (in those with severe hypertension) and atenolol,
while more effective than losartan for mild to moderate hypertension.
化学的特性
Crystalline Solid
使用
For the treatment of hypertension, as well as diabetic nephropathy with an elevated serum creatinine and proteinuria (>300 mg/day) in patients with type 2 diabetes and hypertension. Irbesartan is also used as a second line agent in the treatment of conges
定義
ChEBI: A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
一般的な説明
Irbesartan, 2-butyl-3-[[29-(1H-tetrazol-5-yl)[1,19-biphenyl]-4-yl]methyl]1,3-diazaspiro[4,4]non-1en-4-one (Avapro), like losartan, possesses the acidic tetrazolesystem, which most likely plays a role, similar to the acidicgroups of angiotensin II, in binding to the angiotensin II receptor.In addition, the biphenyl system that serves to separatethe tetrazole from the aliphatic nitrogen is still present.A major difference in this agent is that it does not possessthe acidic side chain. Even so, irbesartan has good affinityfor the angiotensin II receptor because of hydrogen bondingwith the carbonyl moiety of the amide system. Also, thisparticular agent does not require metabolic activation ascandesartan does.
イルベサルタン 上流と下流の製品情報
原材料
準備製品