乙胺痉平
中文名称:
乙胺痉平
中文同义词:
贝那替秦;苯羟乙胺盐酸盐;胃乐康;乙胺痉平;盐酸贝那替秦;盐酸苯那辛;盐酸贝那替嗪;2-(二乙氨基)乙基二苯乙醇酸酯 盐酸盐
英文名称:
BENACTYZINE HYDROCHLORIDE
英文同义词:
2-(diethylamino)-ethanobenzilatehydrochloride;2-(difenyl-hydroxyacetoxy)ethyl-diethylammoniumchlorid;Benactyzine HCL;BENACTYZINE HYDROCHLORIDE 98+%;BENACTYCIN HYDROCHLORIDE;2-(Diethylamino)ethyl benzilate hydrochloride, Benactyzine, α-Hydroxy-α-phenylbenzeneacetic acid 2-(diethylamino)ethyl ester;Amizyl;2-(Difenyl-hydroxyacetoxy)ethyl-diethylammoniumchlorid [czech]
CAS号:
57-37-4
分子式:
C20H26ClNO3
分子量:
363.88
EINECS号:
200-324-4
相关类别:
小分子抑制剂;医药中间体;小分子抑制剂，天然产物;中药对照品;标准品;药物杂质及中间体;Inhibitors;Amines;Aromatics;Intermediates Fine Chemicals;Pharmaceuticals
Mol文件:
57-37-4.mol
熔点
177-179 °C(lit.)
储存条件
Keep in dark place,Sealed in dry,Room Temperature
颜色
Crystals from Me2CO
Merck
14,1029
CAS 数据库
57-37-4(CAS DataBase Reference)
EPA化学物质信息
Benzeneacetic acid, .alpha.-hydroxy-.alpha.-phenyl-, 2-(diethylamino)ethyl ester, hydrochloride (57-37-4)
生物活性
Benactyzine hydrochloride是中枢性毒蕈碱受体拮抗剂。在抑郁症和相关焦虑的治疗中，它被用作抗抑郁剂。
靶点
Target Value
Muscarinic receptor
()
Target
Value
Muscarinic receptor
()
体外研究
Benactyzine hydrochloride and drofenine are widely used anticholinergic drugs which are also competitive inhibitors of BChE with K i values of 0.010±0.001 and 0.003±0.000 mM, respectively. Results indicate that the inhibition of BChE by Benactyzine hydrochloride is pure or partial competitive. Pure competitive inhibition can be distinguished from partial competitive inhibition by plotting v vs [Benactyzine] at a fixed [BTCh].
体内研究
Benactyzine hydrochloride (1 mg/kg) does not influence the attention response. Benactyzine hydrochloride increases the duration of the exploratory-motor reaction, but slightly diminishes the salivation elicited by acetylcholine. There is no blocking effect of Benactyzine hydrochloride and promazine on the EEG-seizure activity elicited by acetylcholine, and almost no inhibitory effect on emotional reactions. Emotional reactions are blocked by high doses of imipramine and promazine, but not by Benactyzine hydrochloride. The data indicates that imipramine, promazine and Benactyzine hydrochloride influence the autonomic effects of serotonin in different ways. Promazine, and especially Benactyzine hydrochloride, inhibit and shorten the period of salivation elicited by the intra-amygdaloid injection of serotonin.
化学性质
白色或几乎白色结晶性粉末。熔点177-181℃。25℃时100ml水中可溶解该品14.9g，几乎不溶于乙醚。无臭，味微苦。其碱基（[302-40-9]）熔点51℃。
用途
抗胆碱药。
生产方法
由二苯乙醇酸与1-氯-2二乙氨基乙烷反应得到。将甲苯、二苯乙醇酸和1-氯-2-二乙氨基乙烷在反应锅内加热回流3h，冷却结晶，甩滤得到的粗品经精制即为该品。
类别
有毒物品
毒性分级
高毒
急性毒性
口服-大鼠 LD50; 184 毫克/公斤; 口服-小鼠 LD50: 160 毫克/公斤
可燃性危险特性
燃烧产生有毒氮氧化物和氯化氢烟雾;极少量服用则精神失常
储运特性
通风低温干燥; 与库房食品原料分开存放
灭火剂
干粉,泡沫,沙土,二氧化碳, 雾状水
危险品标志
T
危险类别码
23/24/25
安全说明
36/37/39-45
危险品运输编号
UN 2811 6.1/PG 3
WGK Germany
3
RTECS号
DD2800000
HazardClass
6.1(b)
PackingGroup
III
毒性
LD50 orl-rat: 184 mg/kg TXAPA9 1,42,59
