Ropinirole hydrochloride

SKU: orb1305289

Description

Ropinirole hydrochloride

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 91374-20-8
• MW: 296.84
• Purity: 99.98%
• Formula: C₁₆H₂₄N₂O·HCl
• SMILES: CCCN(CCC)CCc1c2CC(=O)Nc2ccc1.Cl
• Target: Dopamine Receptor
• Solubility: DMSO:5.63 mg/mL (18.97 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.37 mM);H2O:29.7 mg/mL (100.05 mM)

Bioactivity

• Target IC50:
  D4.4 receptor (human):6.8 (pEC50)|D3 receptor (human):8.4 (pEC50)|D2 receptor:29 nM(Ki)|D2 receptor (human):7.4 (pEC50)
• 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 inhibit 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 int the striatum o the rat causes marked, contralateral (away fro 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.) improve 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. Sinc the major route of elimination for Ropinirole is b the CYP enzyme system, mainly by CYP1A2 and also by CYP3A4, Inhibition o the former and possibl the latter may reduc 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:
  Ropinirole scavenges free radicals and suppresses lipid peroxidation in the Fe2+–Water2 reaction system.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

SKF 101468 hydrochloride, SKF 101468 Hydrochloride, SKF101468, SKF-101468, SKF101468 Hydrochloride, SKF-101468 Hydrochloride, SKF-101468A, Ropinirole, Ropinirole HCl, Ropinirole Hydrochloride, Ropinirole hydrochloride, SKF 101468, disease, DopamineReceptor, Dopamine Receptor, Dopamine, D2, inhibit, Parkinson's, Inhibitor

Compound Identifiers

PubChem CID

68727