罗替戈汀 T6647

Product Introduction
Bioactivity


英文名: Rotigotine-

描述: Rotigotine (N-0923) 是多巴胺受体激动剂，是5-HT1A receptor 的部分激动剂，以及α2B-肾上腺素受体的拮抗剂，用于治疗帕金森病和不宁腿综合征。

激酶实验: Binding assays are performed in 96-well polypropylene tubes in a final volume of 2?mL for D1 and D4 membranes and 1?mL for D2, D3 and D5 membranes containing: 50?μL radioligand, 10?μL drug/buffer/non-specific binding, buffer (final concentration 50?mM Tris-HCl pH 7.4, MgCl2 2?mM) and membranes (5?μg protein for D2 and D3 and 25?μg protein for D1 and D5). Following 120?min of incubation at 25°C, bound radioligand is determined by rapid vacuum filtration through A/C glass fibre filters presoaked in 0.1% polyethylenimine. The filters are washed four times with 2?mL ice-cold ishing buffer (Tris-HCl 50?mM, pH?7.4 at 4°C) and retained radioactivity is determined by liquid scintillation counting.

体外活性: The selectivity of Rotigotine for D3 (pKi 9.2) receptors is higher 10-fold than D2/D4/D5 (pKi 8.5-8.0) and 100-fold than D1 receptors (pKi 7.2). Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. In functional studies, Rotigotine behaves as a full agonist at all dopamine receptors but notably, the potency for stimulation of D1 receptors is similar to that for D2/D3 receptors (pEC50 respectively: 9.0, 9.4-8.6, 9.7). Rotigotine (0.01 μM) slightly protects dopaminergic neurons against MPP+ toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.

体内活性: In primed rats, Rotigotine (0.035/0.1/0.35 mg/kg) dose-dependently induces contralateral turning behavior. In drug-naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 59 mg/mL (187 mM)
Ethanol : 59 mg/mL (187 mM)


关键字: Rotigotine | dopamine | 5-HT1A | Adrenergic Receptor | receptor | N0437 | Serotonin Receptor | 5-HT Receptor | Beta Receptor | N 0437 | N0923 | 5-hydroxytryptamine Receptor | Dopamine Receptor | α2B-adrenergic | Inhibitor | SPM962 | Rotigotine- | inhibit | SPM-962 | N 0923

相关产品: Desipramine hydrochloride | CLOZAPINE N-OXIDE | D4R agonist-1 | SKF-83566 | D3R ligand 1 | Pimozide-d4 | Rotigotine Hydrochloride | Itopride hydrochloride | Ro 10-5824 dihydrochloride | LE 300

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | GPCR Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Orally Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途