盐酸西替利嗪
中文名称:
盐酸西替利嗪
中文同义词:
西替利嗪盐酸盐;盐酸西替利嗪, 一种选择性组胺H1受体拮抗剂;盐酸西替立嗪;(+/-)-2-[2-[4-[(4-氯苯基)苯甲基]-1-哌嗪基]乙氧基]乙酸二盐酸盐;盐酸西替利嗪;盐酸西替利嗪(标准品);盐酸西替利嗪溶液,100PPM;盐酸西替利嗪 1KG
英文名称:
Cetirizine hydrochloride
英文同义词:
(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)aceticaciddihydro;2-[2-[4-[(4-chlorophenyl)-phenyl-methyl]piperazin-1-yl]ethoxy]acetic acid dihydrochloride;Cetirizine Hydrochloride (250 mg);Alercet;Alerid;Cesta;Cetiriz;Cetrak
CAS号:
83881-52-1
分子式:
C21H26Cl2N2O3
分子量:
425.35
EINECS号:
620-533-8
相关类别:
药物原料;中药对照品;标准品;原料;医药原料;小分子抑制剂;中间体;原料药;细胞生物学;API;Aromatics, Heterocycles, Metabolites Impurities, Pharmaceuticals, Intermediates Fine Chemicals;DOPRAM;心脑血管类科研原料药;细胞信号和神经生物学;添加剂;原料;标准品 -中药标准品;化工中间体工业原料;医药原料药;添加剂;有机化学;Active Pharmaceutical Ingredients;Intermediates Fine Chemicals;Pharmaceuticals;Histamine receptor;Aromatics;Heterocycles;Metabolites Impurities
Mol文件:
83881-52-1.mol
熔点
110-115°C
储存条件
Desiccate at RT
溶解度
H2O: soluble5mg/mL, clear
形态
powder
颜色
white to beige
水溶解性
Soluble in water, DMSO, ethanol, and methanol.
Merck
14,2022
InChIKey
PGLIUCLTXOYQMV-UHFFFAOYSA-N
CAS 数据库
83881-52-1(CAS DataBase Reference)
EPA化学物质信息
Acetic acid, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, hydrochloride (1:2) (83881-52-1)
抗过敏药
盐酸西替利嗪是安他乐的羟基衍生物，是一种抗过敏药，是新一代H1受体拮抗剂，属第二代H1抗组胺药，无抗胆碱和抗5-羟色胺的作用，极少透过血脑屏障。对不 同化学诱导性介质包括血管活性多肽、P物质及神经肽等和嗜酸性粒细胞趋化反应有抑制作用，口服见效快，作用强而持久。副作用轻微，表现为嗜睡、疲劳，表情 淡漠、注意力不集中等，一般不必停药。临床上用于治疗季节性或常年性过敏性鼻炎、由过敏原引起的荨麻疹及皮肤瘙痒，用法用量：成人和12岁以上者每次 10 mg，儿童0.1～0.5 mg/kg·d，每日1次。从2008年1月11日起，我国将盐酸西替利嗪由处方药转换为非处方药。在香港以治敏速的名字由葛兰素史克以非处方药发售 。
西替利嗪的有效成分旋西替利嗪是盐酸西替利嗪的光学异构体之一（左旋体）。ChemicalBook andy 整理编辑。
生物活性
Cetirizine DiHCl (UCB P071) 是一种抗组胺剂。
靶点
Target Value
Histamine receptor
Target
Value
Histamine receptor
体外研究
Cetirizine (>5 μM) at higher concentrations can reduce the release of GM-CSF and IL-8 from A549 cells stimulated with IL-1β. Cetirizine exerts anti-inflammatory effects beyond histamine H1-receptor antagonist [2] .
Cell Viability Assay [2]
Cell Line: Human airway epithelial cell line A549.
Concentration: 0-10 μM.
Incubation Time: 24 h.
Result: The survival of A549 cells incubated with various concentrations of cetirizine (0.1, 1, 2.5, 5, and 10 μM) for 24 hours were all higher than 90% when comparing with the control group by MTT test.
Cetirizine, 5 and 10 μM, suppressed GM-CSF release by 70.71 and 61.55%, respectively.
Preincubation with cetirizine, 10 μM, suppressed the IL-8 secretion by 75.04%.
Cell Line:
Human airway epithelial cell line A549.
Concentration:
0-10 μM.
Incubation Time:
24 h.
Result:
The survival of A549 cells incubated with various concentrations of cetirizine (0.1, 1, 2.5, 5, and 10 μM) for 24 hours were all higher than 90% when comparing with the control group by MTT test.
Cetirizine, 5 and 10 μM, suppressed GM-CSF release by 70.71 and 61.55%, respectively.
Preincubation with cetirizine, 10 μM, suppressed the IL-8 secretion by 75.04%.
体内研究
Cetirizine (20 mg/kg, mice, orally) exerts its anti-inflammatory effects by inhibiting MIF as well as IL-8 production in mice immunized and challenged with ragweed pollen [3] .
Animal Model: Male 8-week-old BALB/c mice (25-30 g) immunized and challenged with ragweed pollen [3] .
Dosage: 2 or 20 mg/kg.
Administration: Orally, diluted in sterile water on days 18, 19, and 20.
Result: The neutrophilia at 8 h and eosinophilia at 24 h induced by ragweed pollen extract per os were significantly reduced in the mice treated with 20 mg/kg. The dosage with 2 mg/kg had no effect.
Animal Model:
Male 8-week-old BALB/c mice (25-30 g) immunized and challenged with ragweed pollen [3] .
Dosage:
2 or 20 mg/kg.
Administration:
Orally, diluted in sterile water on days 18, 19, and 20.
Result:
The neutrophilia at 8 h and eosinophilia at 24 h induced by ragweed pollen extract per os were significantly reduced in the mice treated with 20 mg/kg. The dosage with 2 mg/kg had no effect.
用途
主要用于呼吸系统、皮肤和眼睛的过敏性疾病
危险品标志
Xn,Xi
危险类别码
22-36/37/38
安全说明
26-36
危险品运输编号
3249
WGK Germany
3
RTECS号
AG0977500
HazardClass
6.1(b)
PackingGroup
III
海关编码
29339900
