氰美马嗪
| 中文名称 | 氰美马嗪 |
|---|---|
| 中文同义词 | 氰美马嗪;氰美马嗪杂质;赛马咪嗪;赛马咪嗪杂质;西阿米嗪;化合物 T15026;10-(3-(二甲基氨基)-2-甲基丙基)-10H-吩噻嗪-2-甲腈 |
| 英文名称 | cyamemazine |
| 英文同义词 | Cianatil;Kyamepromazine;RP-7204;TH-2602;10-[3-(dimethylamino)-2-methyl-propyl]phenothiazine-2-carbonitrile;10-[3-(dimethylamino)-2-methylpropyl]phenothiazine-2-carbonitrile;10-[3-(DiMethylaMino)-2-Methylpropyl]-10H-phenothiazine-2-carbonitrile;2-Cyano-10-(3-diMethylaMino-2-Methylpropyl)phenothiazine |
| CAS号 | 3546-03-0 |
| 分子式 | C19H21N3S |
| 分子量 | 323.46 |
| EINECS号 | 222-594-2 |
| 相关类别 | 化工原料;Amines;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds |
| Mol文件 | 3546-03-0.mol |
| 结构式 |  |
氰美马嗪 性质
| 熔点 | 90-95°C |
|---|---|
| 沸点 | bp0.2-0.5 205-220° |
| 密度 | 1.21±0.1 g/cm3(Predicted) |
| 储存条件 | Refrigerator |
| 溶解度 | 二甲基亚砜：≥5mg/mL |
| 酸度系数(pKa) | 9.31±0.28(Predicted) |
| 形态 | 粉末 |
| 颜色 | 淡黄色至黄绿色 |
|
5-HT 2A Receptor 1.5 nM (Ki) |
5-HT 2C Receptor 12 nM (Ki) |
5-HT 3 Receptor 75 nM (Ki) |
Cyamemazine exhibits a high affinity for dopamine receptors, which is consistent with its antipsychotic activity. The antagonist activity of Cyamemazine at muscarinic receptors is consistent with its affinity for M 1 ( K i = 13 nM), M 2 ( K i = 42 nM), M 3 ( K i = 321 nM), M 4 ( K i = 12 nM), and M 5 ( K i = 35 nM) receptors.
Cyamemazine behaves as an antagonist at the 5-HT 3 , 5-HT 2C , and 5-HT 2A receptors in 5-HT 3 -dependent contraction of isolated guinea pig ileum and bradycardic responses in rats, in 5-HT 2C -dependent phospholipase C stimulation in the rat brain membrane, and in 5-HT 2A -dependent contraction of isolated rat aorta rings and isolated guinea pig trachea. Cyamemazine antagonizes 5-HT 3 and 5-HT 2C receptors and that this effect is partially involved in its therapeutic activity in anxiety disorders. Acute administration of low doses of Cyamemazine can reduces extracellular dopamine and metabolite concentrations in rat striatum.