For research use only.
Catalog No.S3189 Synonyms: SKF-101468A
CAS No. 91374-20-8
Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
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|Description||Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.|
Ropinirole scavenges free radicals and suppresses lipid peroxidation in the Fe2+–H2O2 reaction system. 
|In vivo||Ropinirole (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.  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.  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.  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.  Ropinirole (0.25 mg-4.0 mg per day) treatment significantly improves patients' ability to initiate sleep, the amount of stage 2 sleep and sleep adequacy compared with placebo. Periodic limb movements with arousal per hour decreases from 7.0 to 2.5 with ropinirole but increases from 4.2 to 6.0 with placebo. Periodic limb movements while awake per hour decreases from 56.5 to 23.6 with ropinirole but increases from 46.6 to 56.1 with placebo. |
|In vitro||Water||60 mg/mL (202.12 mM)|
|DMSO||10 mg/mL (33.68 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03708237||Suspended||Drug: Ropinirole|Drug: Gabapentin|Drug: Placebos||Restless Legs Syndrome|End Stage Renal Disease||University of Alberta||February 19 2019||Phase 2|
|NCT03250117||Terminated||Drug: Ropinirole oral product|Drug: Ropinirole Implant||Parkinson Disease||Titan Pharmaceuticals||October 10 2017||Phase 1|Phase 2|
|NCT00823836||Completed||Drug: ropinirole PR/XR|Drug: ropinirole IR||Parkinson Disease||GlaxoSmithKline||March 2009||Phase 3|
|NCT00530790||Completed||Drug: ropinirole controlled release (CR)-RLS||Restless Legs Syndrome||GlaxoSmithKline||August 23 2007||Phase 2|
|NCT00460148||Completed||Drug: Ropinirole||Parkinson Disease||GlaxoSmithKline||April 2007||Phase 2|
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