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Rotigotine-
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rotigotine-图片
CAS NO:99755-59-6
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Neupro
N-0923
SPM 962
罗替戈汀
N-0437
产品介绍
Rotigotine 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。

产品描述

Rotigotine is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury.

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.

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.

Cas No.

99755-59-6

分子式

C19H25NOS

分子量

315.47

别名

Neupro;N-0923;SPM 962;罗替戈汀;N-0437

储存和溶解度

H2O:<1 mgml
DMSO:59 mg/mL (187 mM)
Ethanol:59 mg/mL (187 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years