83881-52-1
基本信息
盐酸西替利嗪
西替利嗪
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
AKOS 92015
CETIRIZIN DIHYDROCHLORIDE
CETIRIZINE 2HCL
CETIRIZINE DI HCL
CETIRIZINE DIHYDROCHLORIDE
CETIRIZINE HCL
CETIRIZINE HYDROCHLORIDE
ZYRTEC
(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)aceticaciddihydro
(2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-aceticacidihyd
ucb-p071
(±)-2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-acetic acid,dihydrochloride
Cetirazine dihydrochloride
[2-[4-[(4-Chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic Acid, Dihydrochloride
Certirizine
CETIRZINE HYDROCHLORIDE
[83881-51-0], C21H25ClN2O3,388.89
1-piperazinyl]ethoxy]-,dihydrochloride
Acetic acid, [2-[4-[(4-chlorophenyl)phenylmethyl]-
物理化学性质
| 熔点 | 110-115°C |
| 储存条件 | 2-8°C |
| 溶解度 | H2O:可溶5mg/mL,澄清 |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| 水溶解性 | Soluble in water, DMSO, ethanol, and methanol. |
| Merck | 14,2022 |
| BCS Class | 1,3 |
| 稳定性 | 吸湿性 |
| InChI | InChI=1S/C21H25ClN2O3.ClH/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26;/h1-9,21H,10-16H2,(H,25,26);1H |
| InChIKey | PGLIUCLTXOYQMV-UHFFFAOYSA-N |
| SMILES | O=C(COCCN1CCN(C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)CC1)O.[H]Cl |
| 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) |
安全数据
| 危险性符号(GHS) | ![]() GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302 |
| 防范说明 | P264-P270-P301+P312+P330-P501 |
| 危险品标志 | Xn |
| 危险类别码 | R22 |
| 安全说明 | 26-36 |
| 危险品运输编号 | 3249 |
| WGK Germany | 3 |
| RTECS号 | AG0977500 |
| 危险等级 | 6.1(b) |
| 包装类别 | III |
| 海关编码 | 29339900 |
| 存储类别 | 11 - Combustible Solids |
| 危险性类别 | Acute Tox. 4 Oral |
应用领域
制备方法
83881-51-0
83881-52-1
以2-[2-[4-[(4-氯苯基)苯甲基]-1-哌嗪基]乙氧基]乙酸为原料合成盐酸西替利嗪的一般步骤:将2-{2-[4-[(4-氯苯基)苯基甲基]-1-哌嗪基]-乙氧基}乙酸(13.4g,0.034mol)悬浮于丙酮(150ml)中,加热至50℃。在剧烈搅拌下缓慢加入浓盐酸(6.2ml,0.078mol)。反应混合物在室温下继续搅拌2小时,期间逐渐形成2-{2-[4-[(4-氯苯基)苯基甲基]-1-哌嗪基]乙氧基}乙酸二盐酸盐的细白色沉淀。反应完成后,过滤收集沉淀,用丙酮(50ml)洗涤,随后在真空条件下干燥,得到13.8g(产率87.9%)的2-{2-[4-[(4-氯苯基)苯基甲基]-1-哌嗪基]乙氧基}乙酸二盐酸盐,熔点为224-226℃。
参考文献:
[1] Patent: EP1157016, 2003, B1. Location in patent: Page/Page column 5
[2] Patent: US2005/20608, 2005, A1. Location in patent: Page 5-6
[3] Patent: US2004/266787, 2004, A1. Location in patent: Page/Page column 6
常见问题列表
盐酸西替利嗪适用于呼吸系统、皮肤和眼部过敏性疾病,包括常年性变态反应性疾病,如过敏性皮肤病、寻麻疹、过敏性鼻炎、眼瘙痒、眼结膜炎和哮喘等。
本品还用于治疗各种类型皮肤科过敏性疾病。如用于慢性、人工性、寒冷性、迟发压力性、日光性寻麻疹及异位皮炎等的治疗。
本品还是蚊虫叮咬引起的速发性风团和速发性丘团及瘙痒的有效药物。
盐酸西替利嗪不良反应一般轻微,有困倦、嗜睡、头痛、眩晕、激动、口干及胃肠道不适等。偶有天门冬氨酸氨基转移酶轻度升高。
严重的不良反应有:动眼神经危象,表现为两眼向上或向一侧窜动的不自主眼肌痉挛动作等症状。
使用盐酸西替利嗪口服剂型可能会发生嗜睡、眩晕,司机及从事危险操作者应谨慎使用。
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。
| Target | Value |
| Histamine receptor |
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%. |
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. |
知名试剂公司产品信息
盐酸西替利嗪价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2026/06/06 | C2316 | 盐酸西替利嗪 Cetirizine Dihydrochloride | 83881-52-1 | 5G | 190元 |
| 2026/06/06 | C2316 | 盐酸西替利嗪 Cetirizine Dihydrochloride | 83881-52-1 | 25G | 290元 |
| 2026/06/05 | HY-17042AR | 盐酸西替利嗪 Cetirizine dihydrochloride (Standard) | 83881-52-1 | 10 mg | 310元 |
