Ropinirole HCl

製品コードS3189 バッチS318901

印刷

化学情報

Chemical Structure Synonyms SKF-101468A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H24N2O.HCl
分子量 296.84 CAS No. 91374-20-8
Solubility (25°C)* 体外 Water 60 mg/mL (202.12 mM)
DMSO 10 mg/mL (33.68 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
Caudate nucleus is homogenised in incubation buffer (50 mM Tris-HC1, 10 mM KC1, 2 mM MgC12 and 4 mM CaC12, pH 7.6) and centrifuged at 3.9×103 g for 10 min. Supernatant is discarded and the pellet rehomogenised and centrifuged as above and resuspended in fresh incubation medium. Aliquots of membrane are incubated with 0.1 nM 3H-spiperone (67.6 Ci/mmol) in incubation buffer, in the presence and absence of Ropinirole for 60 min at 25℃ (assay volume 2mL). Specific binding is defined with 1 μM (+)butaclamol. Samples are filtered through Whatman GF/C filters using a Brandel cell harvester and washed with 16 ml ice-cold incubation buffer.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The Food and Drug Administration-approved antipsychotic drug trifluoperazine, a calmodulin antagonist, inhibits viral replication through PERK-eIF2α axis [ Front Microbiol, 2022, 13:979904] PubMed: 36386620

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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