盐酸罗替戈汀
盐酸罗替戈汀 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 | 白色至类白色 |
| 稳定性 | 吸湿性 |
| LogP | 3.1 at 20℃ and pH7 |
| 表面张力 | 72.3mN/m at 1g/L and 20℃ |
盐酸罗替戈汀 用途与合成方法
|
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.
盐酸罗替戈汀 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-A0007 | 盐酸罗替戈汀 | 5 mg | 354 | |
| 2024-11-08 | HY-A0007 | 盐酸罗替戈汀 | 125572-93-2 | 10mM * 1mLin DMSO | 389 |
