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首页 化工产品目录 盐酸罗替戈汀
125572-93-2
盐酸罗替戈汀
产品纠错
CAS号:125572-93-2 | 英文名称:(6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride
分子式 C19H26ClNOS
分子量 352
EINECS号 603-080-0
MDL
Smiles
InChIKey
盐酸罗替戈汀化学百科
基本信息
中文名称 盐酸罗替戈汀
英文名称 (6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride
CAS号 125572-93-2
分子式 C19H26ClNOS
分子量 351.93
EINECS号 603-080-0
物化性质
熔点 114-117°C
密度 1.2g/cm3 at 20℃
蒸气压 0-0Pa at 20-25℃
LogP 3.1 at 20℃ and pH7
溶解度 可溶于丙酮(轻微、加热、超声处理)、DMSO(轻微)、甲醇(轻微)
形态 固体
颜色 白色至类白色
稳定性 吸湿性
安全信息
WGK Germany 2
海关编码 2934990002
生产及用途
Rotigotine Hydrochloride (N-0923 Hydrochloride) 是 dopamine receptor 纯激动剂,是 5-HT1A receptor 的部分激动剂,以及 α2B-adrenergic receptor 的拮抗剂,Ki 值分别为 0.71 nM (dopamine D3 receptor),4-15 nM (D2,D5,D4 receptors),83 nM (dopamine D1 receptor)。

D 3 Receptor

0.71 nM (Ki)

D 2 Receptor

4-15 nM (Ki)

D 5 Receptor

4-15 nM (Ki)

D 4 Receptor

4-15 nM (Ki)

D 1 Receptor

83 nM (Ki)

α1A

176 nM (Ki)

α1B

273 nM (Ki)

α2A

338 nM (Ki)

α2B

27 nM (Ki)

5-HT 1A Receptor

30 nM (Ki)

5-HT 7 Receptor

86 nM (Ki)

Rotigotine (N-0923) has a 10-fold selectivity for D3 (pK i 9.2) receptors compared with D2, D4 and D5 (pK i 8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK i 7.2). In functional studies, Rotigotine (N-0923) behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC 50 respectively: 9.0, 9.4-8.6, 9.7). Rotigotine (N-0923) (10 µM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. 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.

In primed rats, Rotigotine (N-0923) (0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.

用途 
It is a non-ergot dopamine agonist drug and is indicated for the treatment of Parkinson鈥檚 disease.
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