1-[2-(3,4-二甲氧基苯基)乙基]-4-(3-苯基丙基)哌嗪盐酸盐
| 中文名称 | 1-[2-(3,4-二甲氧基苯基)乙基]-4-(3-苯基丙基)哌嗪盐酸盐 |
|---|---|
| 中文同义词 | 1-(3,4-二甲氧基苯乙基)-4-(3-苯基丙基)哌嗪双盐酸盐;1-[2-(3,4-二甲氧基苯基)乙基]-4-(3-苯基丙基)哌嗪盐酸盐;库他美新二盐酸盐;1-(3,4-二甲氧基苯乙基)-4-(3-苯丙基)哌嗪双盐酸盐;SA 4503 二盐酸盐 |
| 英文名称 | SA-4503,1-(3,4-DIMETHOXYPHENETHYL)-4-(3-PHENYLPROPYL)PIPERAZINE DIHYDROCHLORIDE |
| 英文同义词 | SA 4503 (dihydrochloride);Cutamesine dihydrochloride;1-[2-(3,4-DiMethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride;SA-4503;SA-4503,1-(3,4-DIMETHOXYPHENETHYL)-4-(3-PHENYLPROPYL)PIPERAZINE DIHYDROCHLORIDE;1-(3,4-Dimethoxyphenethyl)-4-(3-phenylpropyl)piperazinedihydrochloride;1-[2-(3,4-Dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine hydrochloride;SA-4503(2HCl) |
| CAS号 | 165377-44-6 |
| 分子式 | C23H32N2O2.2ClH |
| 分子量 | 441.44 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 165377-44-6.mol |
| 结构式 | ![1-[2-(3,4-二甲氧基苯基)乙基]-4-(3-苯基丙基)哌嗪盐酸盐 结构式](CAS/GIF/165377-44-6.gif) |
1-[2-(3,4-二甲氧基苯基)乙基]-4-(3-苯基丙基)哌嗪盐酸盐 性质
| 熔点 | 250-252°C |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 溶于DMSO（高达5mg/ml）或水（高达至少25mg/ml）。 |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 稳定性 | 自购买之日起 1 年内保持稳定。 DMSO 或蒸馏水中的溶液可在 -20° 下储存长达 1 个月。 |
IC50: 17.4 nM (σ1receptor, guinea pig brain membranes)
The sigma receptor might be involved in several diseases in the central nervous system. Cutamesine, a potent σ1receptor agonist, has 103-fold higher affinity for σ1 (IC 50 =17.4 nM) than σ2 (IC 50 =1,784 nM) sites in guinea pig brain membranes. Cutamesine is 14-fold selective for σ1 (K i =4.6 nM) over σ2 (K i =63.1 nM) sites in guinea pig brain homogenates. Cutamesine protects motor neuron NSC34 cells against superoxide dismutase 1 and serum free neurotoxicity. It upregulates the phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK) 1/2. Cutamesine reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1.
Cutamesine extends the survival time in the SOD1G93A mice.