Ropinirole HCl

For research use only.

Catalog No.S3189 Synonyms: SKF-101468A

Ropinirole HCl Chemical Structure

CAS No. 91374-20-8

Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.

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Biological Activity

Description Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
Targets
D2 receptor [1]
29 nM(Ki)
In vitro

Ropinirole scavenges free radicals and suppresses lipid peroxidation in the Fe2+–H2O2 reaction system. [2]

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. [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] 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. [5]

Protocol

Solubility (25°C)

In vitro Water 60 mg/mL (202.12 mM)
DMSO 10 mg/mL (33.68 mM)
Ethanol Insoluble

* 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.

Chemical Information

Molecular Weight 296.84
Formula

C16H24N2O.HCl

CAS No. 91374-20-8
Storage powder
in solvent
Synonyms SKF-101468A
Smiles CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1.Cl

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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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Dopamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID