氰美马嗪

中文名称:

氰美马嗪

中文同义词:

赛马咪嗪;氰美马嗪;氰美马嗪杂质;赛马咪嗪杂质

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

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 

DMSO: ≥5mg/mL

酸度系数(pKa)

9.31±0.28(Predicted)

形态

powder

颜色

light yellow to yellow-green

生物活性

Cyamemazine 是一种抗精神病药，其中含有吩噻嗪发色团，通常被用作抗焦虑药。Cyamemazine 是具有抗精神病活性的有效的 5-HT3 (Ki 为 12 nM), 5-HT2A (Ki 为 1.5 nM) 和 5-HT2C (Ki 为 75 nM) 受体拮抗剂。

靶点

5-HT 2A Receptor 1.5 nM (Ki) 5-HT 2C Receptor 12 nM (Ki) 5-HT 3 Receptor 75 nM (Ki)

5-HT 2A Receptor 1.5 nM (Ki)

5-HT 2C Receptor 12 nM (Ki)

体外研究

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.

体内研究

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.

危险品标志 

Xi,N

危险类别码 

50

安全说明 

61

危险品运输编号 

UN 3077 9 / PGIII

WGK Germany 

3

毒性

LDLo oral in man: 107mg/kg