ROPINIROLE HCL
Ropinirole hydrochloride
CAS: 91374-20-8
Molecular Formula: C16H25ClN2O
ROPINIROLE HCL - Names and Identifiers
| Name | Ropinirole hydrochloride |
| Synonyms | Requi REQUIP SKF-101468A ROPINIROLE HCL Ropinirol hydrochloride Ropinirole hydrochloride 4-(2-(dipropylamino)ethyl)-2-indolinonemonohydrochloride 4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone Hydrochloride 4-(2-Dipropylaminoethyl)-1,3-dihydroindol-2-one hydrochloride 4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one Hydrochloride 1,3-dihydro-4-(2-(dipropylamino)ethyl)-2h-indol-2-onmonohydrochloride 1,3-dihydro-4-(2-(dipropylamino)ethyl)-2h-indol-2-onemonohydrochloride |
| CAS | 91374-20-8 |
| EINECS | 635-615-9 |
| InChI | InChI=1/C16H24N2O.ClH/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15;/h5-7H,3-4,8-12H2,1-2H3,(H,17,19);1H |
ROPINIROLE HCL - Physico-chemical Properties
| Molecular Formula | C16H25ClN2O |
| Molar Mass | 296.84 |
| Melting Point | 241-243°C |
| Boling Point | 410.5°C at 760 mmHg |
| Flash Point | 202°C |
| Solubility | H2O: >10mg/mL |
| Vapor Presure | 6.01E-07mmHg at 25°C |
| Appearance | powder |
| Color | light yellow |
| Storage Condition | 2-8°C |
| In vitro study | Ropinirole scavenges free radicals and inhibits Fe |
| In vivo study | Ropinirole (50 mg/kg, I. p.) elicits biphasic spontaneous locomotor activity in mice. Ropinirole (0.05-1.0 mg/kg SC) dose-dependently inhibited 2-di-n-propylamino-5, 6-dihydroxytetrahydronaphthalene-induced dyskinesia in mice. Direct unilateral injection of Ropirtirole into the rat striatum at doses of 1 and 10 μg caused significant contralateral (relative to the injected side) asymmetry and gyration in mice. Ropinirole (0.05-1.0 mg/kg SC or 0.1 mg/kg PO) reversed all motor and behavioral deficits induced by MPTP in marmosets. In mice, Ropinirole (2 mg/kg, I. p.) administration for 7 days increased the activities of GSH, catalase and SOD in the striatum and protected striatum dopaminergic neurons from 6-hydroxydopamine (6-OHDA). In dysfunctional rats with D2R and D3R overexpression in the striatum, Ropinirole (0.2 mg/kg, I. p.) improves the use of previously immobile forelimbs and produces strong convoluted behavior. In dysfunctional rats with overexpression of D2R and D3R in the striatum, insufficient Ropinirole treatment produced only moderate stimulation. In healthy volunteers, Ropinirole (1-8 mg t. I. d.) it is rapidly and completely absorbed, has an oral bioavailability of 55%, a clearance of 780 ml/min, and an elimination half-life of 6 hours. Since the main route of Ropinirole clearance is through the CYP enzyme system, mainly through CYP1A2 and CYP3A4, the inhibition of the former may also be the inhibition of the latter, reducing the clearance rate of the reagent, and lead to drug accumulation. Compared to placebo, treatment with Ropinirole (0.25 mg-4.0 mg per day) significantly improved the patient's ability to enter sleep, and the amount of Stage 2 sleep, and adequate sleep. Periodic limb movements per hour during wakefulness decreased from 7.0 to 2.5 in the ropinirole group and increased from 4.2 to 6.0 in the placebo group. Cyclic limb movements per hour during wakefulness decreased from 56.5 to 23.6 in the ropinirole group and increased from 46.6 to 56.1 in the placebo group. |
ROPINIROLE HCL - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R50/53 - Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. R36/38 - Irritating to eyes and skin. |
| Safety Description | S36 - Wear suitable protective clothing. S60 - This material and its container must be disposed of as hazardous waste. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. S37/39 - Wear suitable gloves and eye/face protection S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 3077 9/PG 3 |
| WGK Germany | 3 |
| RTECS | NM3288250 |
| HS Code | 2933790002 |
ROPINIROLE HCL - Reference Information
| indication | is mainly used for the treatment of early idiopathic Parkinson's disease. |
| pharmacological action | ropinirole hydrochloride is a dopamine D2 receptor agonist, it is a selective non-ergoline dopamine D2 receptor agonist. Unlike other dopamine agonists, this product has a simple chemical structure very similar to natural dopamine, acting on postsynaptic receptors in the striatum, compensating for the lack of dopamine, compensating for increased sympathetic tone. Ropinirole can also be used as an adjunctive therapy in patients who have already experienced a switch phenomenon. It can directly act on synaptic receptors to produce continuous stimulation, thereby easing the movement fluctuation of L-dopa, reducing the difficulty of its action and reducing the dosage. Dopamine receptors are divided into D1 and D2 a total of 1 subtypes, when the dopamine agonist and D1 receptor binding, the complex will activate adenosyl cyclase, increase the formation of cyclic adenosine phosphate, so as to promote the transmission of information between nerve cells, but the advantages and disadvantages of this role remains to be further studied. In contrast, when an agonist binds to the D2 receptor, it is possible to inhibit adeno-cyclase or have no effect on it. D2 receptors are located in the striatum which is thought to be associated with the anti-dopa agonistic effect. |
| pharmacokinetics | The oral bioavailability of ropinirole hydrochloride was approximately 50%. When the oral dose was 1.0~5.0mg, the plasma Cmax was proportional to the dose, and the tmax was 1.5h. No accumulation in the body, mainly by oxidative metabolism, urinary excretion. Mild to moderate renal dysfunction, without dose adjustment. The clearance time was about 3.5h. |
| biological activity | Ropinirole (SKF-101468A) is a selective D2 receptor inhibitor with an IC50 of 29 nM. |
| Target | Value |
| D2 receptor | 29 nM(Ki) |
| Use | indication: for the treatment of Parkinson's disease |
Last Update：2024-04-10 22:29:15
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Product Name: Ropinirole HCl Visit Supplier Webpage Request for quotationCAS: 91374-20-8
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Ropinirole Hydrochloride Visit Supplier Webpage Request for quotationCAS: 91374-20-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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