盐酸丙咪嗪

中文名称:

盐酸丙咪嗪

中文同义词:

盐酸丙咪嗪溶液, 100PPM;N,N-二甲基-10,11-二氢-5H-二苯并[b,f]氮杂卓-5-丙胺盐酸盐;盐酸丙咪嗪;托弗尼尔;丙咪嗪盐酸;丙咪嗪盐酸盐;丙咪嗪;咪帕明

英文名称:

Imipramine hydrochloride

英文同义词:

Imipramine hydrochloride,10,11-Dihydro-N,N-dimethyl-5H-dibenz[b,f]azepine-5-propanamine hydrochloride, 5-[3-(Dimethylamino)propyl]-10,11-dihydro-5H-dibenz[b,f]azepine hydrochloride;Imipramine Hydrochloride (200 mg);Methanol(test Imipramine HCl, 1.0 mg/mL as free base);10,11-Dihydro-N,N-dimithyl-5,H-dibenz[b,f]azepine-5-propanamine;5-(3-dimethylaminopropyl)-10,11-dihydro-5h-dibenz(b,f)azepinehydrochloride;tofranil;tofranile;LABOTEST-BB LT00452014

CAS号:

113-52-0

分子式:

C19H25ClN2

分子量:

316.87

EINECS号:

204-030-7

相关类别:

药物成分 (研究实验用);医药原料;医药原料药;Intermediates Fine Chemicals;Pharmaceuticals;APIs;Adrenoceptor;API

Mol文件:

113-52-0.mol

熔点 

168-1700C

闪点 

9℃

储存条件 

2-8°C

溶解度 

H2O: 50 mg/mL

形态

crystalline

颜色

white

PH值

4.2～5.2(100g/l,25℃)

水溶解性 

Soluble in water

最大波长(λmax)

260nm(lit.)

Merck 

14,4920

CAS 数据库

113-52-0(CAS DataBase Reference)

EPA化学物质信息

5H-Dibenz[b,f]azepine-5-propanamine, 10,11-dihydro-N,N-dimethyl-, monohydrochloride (113-52-0)

生物活性

Imipramine hydrochloride 抑制血清素转运蛋白(serotonin)，IC50 值为 32 nM。Imipramine hydrochloride 可阻止胰酶的易位，抑制 MV 和外泌体的分泌。

靶点

IC50: 32 nM (serotonin)

体外研究

Depression-like behavior is often complicated by chronic pain. Antidepressants including imipramine are widely used to treat chronic pain, but the mechanisms are not fully understood. Imipramine (IC 50 =32 nM) and desipramine (IC 50 =160 nM) are found to be potent inhibitors of the human placental serotonin transporter.

体内研究

Administration of imipramine reverses social avoidance behavior, significantly increasing the interaction time. 24 days of imipramine treatment in RSD mice significantly decreases stress-induced mRNA levels for IL-6 in brain microglia. Chronic mild stress induces a long-term altered gene expression profile in the prefrontal cortex that is partially reverted by imipramine treatment (10mg/kg, i.p.). Chronic imipramine administration alteres the amino acid dynamics in the brain. In the striatum, the concentrations of asparagine, glutamine and methionine are significantly increased by chronic imipramine administration. In the thalamus and hypothalamus, chronic imipramine administration significantly decreased the valine concentration. Imipramine reduces pain-related negative emotion without influencing pain and that this effect is diminished by denervation of 5-HT neurons and by anti-BDNF treatment. Imipramine also normalizes derangement of ERK/CREB coupling, which leads to induction of BDNF. This suggests a possible interaction between 5-HT and BDNF. Imipramine treatment counteracts the corticosterone administration-induced increase in the reactivity of rat CA3 hippocampal circuitry to the activation of the 5-HT receptor.

化学性质 

白色结晶性粉末。熔点174-175℃。易溶于水、乙醇，微溶于丙酮，几乎不溶于乙醚。无臭，味苦。遇光渐变色。米帕明碱（[50-49-7]）沸点160℃（13.3Pa）。

用途 

镇静安眠性抗组织胺及抗抑郁药，治疗精神抑郁症及小儿遗尿症。

用途 

用于治疗各种类型抑郁症、小儿遗尿症等

生产方法 

10，11-二氢-5-二苯并[b，f]氮杂卓（见14230）与甲苯、钠氨一起加热回流1h，冷至40-50℃，滴加1-氯-3-二甲氨基丙烷，再回流16h。冷却，过滤，滤液水洗层，取甲苯层减压蒸馏，回收甲苯后，收集210-230℃（0.67kPa）馏分，得米帕明碱，最后经成盐而得成品。

危险品标志 

Xn,T,F

危险类别码 

23/25-36/38-36/37/38-22-39/23/24/25-23/24/25-11

安全说明 

7-16-24-33-45-36-26-36/37

危险品运输编号 

UN 1230 3/PG 2

WGK Germany 

3

RTECS号

HO1925000

TSCA 

Yes

海关编码 

2933995800

毒性

LD50 in mice, rats (mg/kg): 400, 490 orally; 110, 90 i.p. (Tobe)