5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐

5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐

中文名称5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐
中文同义词5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐;盐酸罗替高汀;罗替高汀-D7盐酸;消旋罗替戈汀;罗替高汀消旋体;化合物 T12676;6-(PROPYL(2-(THIOPHEN-2-YL)ETHYL)AMINO)-5,6,7,8-TETRAHYDRONAPHTHALEN-1-OL HYDROCHLORIDE
英文名称rac-Rotigotine Hydrochloride
英文同义词rac-Rotigotine Hydrochloride;1-Naphthalenol,5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-,hydrochloride;N 0437 hydrochloride;5,6,7,8-Tetrahydro-6-[propyl[2-(2-thienyl)ethyl]aMino]-1-naphthalenol Hydrochloride;1-Naphthalenol, 5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]aMino]-, (Hydrochloride) (1:1);Rotigotine Impurity 2(Rotigotine Racemate HCl);Rotigotine-d7 HCl;(Rac) Rotigotine hydrochloride,(Rac)Rotigotine hydrochloride
CAS号102120-99-0
分子式C19H26ClNOS
分子量351.93
EINECS号
相关类别Aromatics;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds
Mol文件102120-99-0.mol
结构式5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐 结构式

5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐 性质

熔点>118°C (dec.)
储存条件Refrigerator
溶解度可溶于丙酮、DMSO、甲醇
形态固体
颜色白色至类白色

5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐 用途与合成方法

(Rac)-Rotigotine hydrochloride 是 Rotigotine 的外消旋体。Rotigotine 是 dopamine receptor 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

13.5 nM (Ki)

D 4 Receptor

3.9-15 nM (Ki)

D 5 Receptor

5.4 nM (Ki)

D 1 Receptor

83 nM (Ki)

5-HT 1A Receptor

30 nM (Ki)

5-HT 2B Receptor

27 nM (Ki)

Rotigotine 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 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 (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. .

安全信息

海关编码2934990002

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-15394(Rac)-Rotigotine hydrochloride5 mg400元
2024/01/25HY-153945,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐
(Rac)-Rotigotine hydrochloride
102120-99-010mg640元

5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐 上下游产品信息

"5,6,7,8-四氢-6-[丙基[2-(2-噻吩基)乙基]氨基]-1-萘酚盐酸盐"相关产品信息
2-甲基吲哚 正丙苯 硅烷
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