盐酸氯吡胺
中文名称:
盐酸氯吡胺
中文同义词:
N-(4-氯苄基)-N,N-二甲基-N-2-吡啶基-1,2-乙二胺盐酸盐;盐酸氯吡胺;N-(4-氯苄基)-N,N’-二甲基-N-2-吡啶基-1,2-乙二胺;氯吡胺盐酸盐;氯吡拉敏盐酸盐;N-对氯苄基-N′,N′-二甲基-N-(2-吡啶基)乙二胺;盐酸氯吡胺盐
英文名称:
Chloropyramine hydrochloride
英文同义词:
CHLOROPYRAMINE HCL;CHLOROPYRAMINE HYDROCHLORIDE;CHLOROPYRAMINE MONOHYDROCHLORIDE;N-P-CHLOROBENZYL-N,N-DIMETHYL-N-(2-PYRIDYL)ETHYLENEDIAMINE HYDROCHLORIDE;N-P-CHLOROBENZYL-N,N-DIMETHYL-N-[2-PYRIDYL]ETHYLENEDIAMINE HYDROCHLORIDE;N-P-CHLOROBENZYL-N,N-DIMETHYL-N-[2-PYRIDYL]LETHYLENEDIAMINE HYDROCHLORIDE;N1-(4-Chlorobenzyl)-N2,N2-dimethyl-N1-(pyridin-2-yl)ethane-1,2-diamine hydrochloride;Chloropyramine HCI
CAS号:
6170-42-9
分子式:
C16H21Cl2N3
分子量:
326.26
EINECS号:
228-216-2
相关类别:
小分子抑制剂;医药原料
Mol文件:
6170-42-9.mol
熔点
172-174°
储存条件
Inert atmosphere,Room Temperature
形态
neat
CAS 数据库
6170-42-9(CAS DataBase Reference)
生物活性
Chloropyramine hydrochloride 是一种组胺受体 H1 (histamine receptor H1) 拮抗剂，它也能抑制 VEGFR-3 和 FAK 的生化功能。
靶点
VEGFR-3
VEGFR-3
体外研究
BT474 cells are highly sensitive to Chloropyramine hydrochloride (compound 1) treatment, whereby 1 µM concentrations cause a 40% reduction of viability after 48 h of treatment. It is found that at 1 µM concentrations of Chloropyramine hydrochloride, viability of control MCF7-pcDNA3 cells is significantly higher than the viability of MCF7-VEGFR-3 cells (P<0.01) and at 10 µM concentration this difference reaches twofold (P<0.001). In the BT474 cells treatment with Chloropyramine hydrochloride also leads to a concentration-dependent decrease of cell proliferation. When treatment with Chloropyramine hydrochloride is continued for 48 h, the breast cancer cells that overexpressed VEGFR-3 undergo apoptosis. This effect is dose-dependent, with 10 µM Chloropyramine hydrochloride inducing apoptosis in more than 60% of BT474 cells. In our model cell lines MCF7-pcDNA3 and MCF7-VEGFR-3, treatment with 10 µM Chloropyramine hydrochloride for 48 h leads to a 4-fold increase in apoptotic cell death in the cell line that overexpressed VEGFR-3 (18% versus 76 % respectively).
体内研究
Chloropyramine hydrochloride causes a dramatic reduction of tumor growth in both model systems whereby the tumor size in the treated groups is approximately 20% of the tumor size in vehicle control groups. Doxorubicin administered at 3 mg/kg causes approximately 60% reduction of tumor growth, but has no effect on tumor growth at 0, 3 mg/kg. In contrast, there is a modest effect of Chloropyramine hydrochloride alone (50% reduction of tumor growth). The low-dose combination of Chloropyramine hydrochloride and doxorubicin has a prolonged anti-tumor effect (85% reduction of tumor growth) that is greater than either drug alone.
化学性质
类白色至白色结晶性粉末。熔点168-172℃。
用途
抗过敏药。
用途
抗过敏原料药
WGK Germany
3
