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Ropinirole HCl
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Ropinirole HCl图片
CAS NO:91374-20-8
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
25mg电议
50mg电议

产品介绍
Ropinirole (SKF 101468) hydrochloride 是一种口服有效的 D3/D2 受体激动剂，对 D2 受体的 Ki 值为 29 nM。
Cas No.91374-20-8
别名盐酸罗匹尼罗; SKF 101468 hydrochloride
化学名4-[2-(dipropylamino)ethyl]-1,3-dihydroindol-2-one;hydrochloride
Canonical SMILESCCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1.Cl
分子式C16H24N2O.HCl
分子量296.84
溶解度≥ 14.95mg/mL in Water
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ropinirole hydrochloride(SKF101468 hydrochloride) a selective dopamine D2 receptor inhibitor with IC50 of 29 nM.Target: Dopamine D2 ReceptorRopinirole (50 mg/kg, i.p.) causes biphasic spontaneous locomotor activity in mice. Ropinirole (0.05-1.0 mg/kg SC) dose-dependently inhibits the dyskinesias induced by 2-di-n-propylamino-5,6-di-hydroxytetralin in mice. Ropirtirole, at doses of 1 and 10 μg, injected unilaterally directly into the striatum of the rat causes marked, contralateral (away from the side of injection) asymmetry and circling in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reverses all motor and behavioural deficits induced by MPTP in marmosets [1]. Ropinirole (2 mg/kg, i.p.) for 7 days increases GSH, catalase and SOD activities in the striatum and protected striatal dopaminergic neurons against 6-hydroxydopamine (6-OHDA) in mice [2]. Ropinirole (0.2 mg/kg, i.p.) improves the use of previously akinetic forelimb and produced robust circling behavior in lesioned rats with striatal over-expression of both D2R and D3R compared to lesioned animals that received blank vector. The subtherapeutic dose of ropinirole generates only modest motor effects in lesioned rats with sole over-expression of D2R or D3R [3]. Ropinirole (1-8 mg t.i.d.) is rapidly and completely absorbed with oral bioavailability of 55%, clearance of 780 mL/min, elimination half-life of 6 hours in healthy volunteer. Since the major route of elimination for Ropinirole is by the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4, inhibition of the former and possibly the latter may reduce the agent's clearance and lead to drug accumulation [4].

References:
[1]. Eden, R.J., et al., Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist. Pharmacol Biochem Behav, 1991. 38(1): p. 147-54.
[2]. Iida, M., et al., Dopamine D2 receptor-mediated antioxidant and neuroprotective effects of ropinirole, a dopamine agonist. Brain Res, 1999. 838(1-2): p. 51-9.
[3]. Lam, Y.W., Clinical pharmacology of dopamine agonists. Pharmacotherapy, 2000. 20(1 Pt 2): p. 17S-25S.
[4]. Allen, R., et al., Ropinirole decreases periodic leg movements and improves sleep parameters in patients with restless legs syndrome. Sleep, 2004. 27(5): p. 907-14.