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 |
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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 性质
熔点 | 250-252°C |
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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.