Home Neuronal Signaling Dopamine Receptor inhibitor Ropinirole HCl

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Ropinirole HCl Dopamine Receptor inhibitor

Cat.No.S3189

Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
Ropinirole HCl Dopamine Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 296.84

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Chemical Information, Storage & Stability

Molecular Weight 296.84 Formula

C16H24N2O.HCl

 Storage (From the date of receipt)
CAS No. 91374-20-8 Download SDF Storage of Stock Solutions

Synonyms SKF-101468A Smiles CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1.Cl

Solubility

In vitro
Batch:

Water : 59 mg/mL

DMSO : 30 mg/mL (101.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
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]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10641988/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15453549/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03708237 Terminated
Restless Legs Syndrome|End Stage Renal Disease
University of Alberta
 February 19 2019 Phase 2
NCT03250117 Terminated
Parkinson Disease
Titan Pharmaceuticals
 October 10 2017 Phase 1|Phase 2
NCT00823836 Completed
Parkinson Disease
GlaxoSmithKline
 March 2009 Phase 3
NCT00530790 Completed
Restless Legs Syndrome
GlaxoSmithKline
 August 23 2007 Phase 2
NCT00460148 Completed
Parkinson Disease
GlaxoSmithKline
 April 2007 Phase 2

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