Ropinirole hydrochloride

Ropinirole hydrochloride 속성

Ropinirole hydrochloride C화학적 특성, 용도, 생산

개요

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 D₂ agonist with activity in the extrapyramidal system. It has weak or no significant activity at α₂-adrenergic, 5-HT₂ receptors and is inactive at 5-HT₁, benzodiazepine, GABA, α₁ 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.

화학적 성질

Off-White Solid

용도

An antiparkinsonian agent. A selective dopamine D2-receptor agonist

일반 설명

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 D₂ receptors. Ropinirole is indicated for thetreatment of the signs and symptoms of idiopathic PD andmoderate to severe primary RLS.

생물학적 활성

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.

Ropinirole hydrochloride 준비 용품 및 원자재

원자재

준비 용품

Ropinirole hydrochloride 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Hefei TianRui Pharmaceutical Chemical Co., Ltd.	+86-0551-68665055 +86-+86-18616906106	sales@trywchem.com	China	129	58
Shaanxi Haibo Biotechnology Co., Ltd	+undefined18602966907	qinhe02@xaltbio.com	China	1000	58
Henan Fengda Chemical Co., Ltd	+86-371-86557731 +86-13613820652	info@fdachem.com	China	16805	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Shanghai Bojing Chemical Co.,Ltd.	+86-86-02137122233 +8613795318958	bj1@bj-chem.com	China	298	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Shanghai Yingrui Biopharma Co., Ltd.	+86-21-33585366 - 03@	sales03@shyrchem.com	CHINA	738	60
Nanjing Finetech Chemical Co., Ltd.	025-85710122 17714198479	sales@fine-chemtech.com	CHINA	885	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Jinan Shengqi pharmaceutical Co,Ltd	86+18663751872	christine@shengqipharm.com	CHINA	491	58

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