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125572-93-2

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 125572-93-2
分子式 C19H26ClNOS
分子量 351.93
MOL 文件 125572-93-2.mol
更新日期 2024/04/30 11:17:53
125572-93-2 结构式 125572-93-2 结构式

基本信息

中文别名
盐酸罗替戈汀
盐酸罗替戈汀中文同义词:盐酸罗替戈汀
[2H3]-RAC ROTIGOTINE HYDROCHLORIDE SALT
(S)-5,6,7,8-四氢-6-[丙基[2-(2-噻吩)乙基]氨基]-1-萘酚盐酸盐
英文别名
(6S)-
CS-1395
rotigotine HCl
Rotigotine hydrochloride
hydrochloride hcl powder
CEXBONHIOKGWNU-NUDVEOEASA-N
[2H3]-Rac Rotigotine Hydrochloride Salt
8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]aMino]-
(6S)-6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol hydrochloride
(S)-6-(propyl(2-(thiophen-2-yl)ethyl)aMino)-5,6,7,8-tetrahydronaphthalen-1-ol

物理化学性质

熔点114-117°C
密度1.2g/cm3 at 20℃
蒸气压0-0Pa at 20-25℃
储存条件room temp
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
颜色白色至灰白色
稳定性吸湿性
LogP3.1 at 20℃ and pH7
表面张力72.3mN/m at 1g/L and 20℃

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H412-H317-H302
WGK Germany2
海关编码2934990002

应用领域

用途1
It is a non-ergot dopamine agonist drug and is indicated for the treatment of Parkinson鈥檚 disease.
盐酸罗替戈汀价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-A0007盐酸罗替戈汀
Rotigotine Hydrochloride
125572-93-250mg1500元
2024/04/30HY-A0007盐酸罗替戈汀
Rotigotine Hydrochloride
125572-93-210mM * 1mLin DMSO1650元
2024/04/30HY-A0007盐酸罗替戈汀
Rotigotine Hydrochloride
125572-93-2100mg2100元

常见问题列表

生物活性
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)。
靶点

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)

体外研究

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.

体内研究

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.

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