ロピニロール·塩酸塩 化学特性,用途語,生産方法
外観
白色～褐色, 結晶性粉末～粉末
溶解性
水に可溶
効能
パーキンソン病治療薬, ドパミン受容体作動薬
商品名
レキップ (グラクソ・スミスクライン); レキップ (グラクソ・スミスクライン)
説明
ReQuip was launched in the UK as a monotherapy or in combination with
low-dose levodopa for the treatment of early-stage idiopathic Parkinson's disease.
An eight step (24% overall yield) synthesis from isochroman provides access to
ropinirole. It is a non-ergot postsynaptic dopamine D
2 agonist with activity in the
extrapyramidal system. It has weak or no significant activity at α
2-adrenergic, 5-HT
2
receptors and is inactive at 5-HT
1, benzodiazepine, GABA, α
1 and β adrenoreceptors.
Thus it has essentially no CNS side effects, fewer dyskinesias and on-off fluctuations.
In animals, it was able to reverse all motor deficits induced by MPTP. Tolerance is
not developed and ropinirole has similar postsynaptic potency to apomorphine but
with significantly less stereotyped behavior.
化学的特性
Off-White Solid
使用
An antiparkinsonian agent. A selective dopamine D2-receptor agonist
一般的な説明
Ropinirole hydrochloride,4-(2-(dipropylamino)ethyl)indolin-2-one hydrochloride(Requip), is a white to pale greenish yellow powder that isvery soluble in water. Ropinirole is rapidly absorbed afteroral administration with maximal plasma concentrationsgenerally reached after about 1.5 hours, and the eliminationhalf-life appears to be approximately 3 hours. Ropinirole isalso rapidly and extensively distributed from the vascularcompartment and shows low plasma protein binding that isindependent of its plasma concentration. This drug iscleared by metabolism in the liver, with only 10% being excretedunchanged. The main metabolite of ropinirole is theN-despropyl metabolite. The glucuronide of this metaboliteand the carboxylic acid metabolite, 4-carboxymethylindolin-2-one, account only for 10% of the administered dose.None of the metabolites is pharmacologically active, and theexcretion of ropinirole-derived products is mainly via theurine. The main CYP450 isozyme involved in the metabolismof ropinirole is CYP1A2. Inhibitors or inducers ofthis enzyme have been shown to alter the clearance ofropinirole.Ropinirole is believed to act as an agonist atpostsynaptic D
2 receptors. Ropinirole is indicated for thetreatment of the signs and symptoms of idiopathic PD andmoderate to severe primary RLS.
生物活性
Selective D 2 -like receptor agonist (D 3 > D 2 > D 4 ). Causes biphasic spontaneous locomotor activity and contralateral circling in 6-OHDA-lesioned mice. Displays antiParkinsonian activity.
ロピニロール·塩酸塩 上流と下流の製品情報
原材料
準備製品