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盐酸西替利嗪

盐酸西替利嗪用途

Cetirizine二盐酸盐是第二代抗组胺剂,是hydroxyzine的主要代谢产物,是外消旋的选择性H1受体反向激动剂。

盐酸西替利嗪名称

[ CAS 号 ]:
83881-52-1

[ 中文名 ]:
盐酸西替利嗪

[ 英文名 ]:
Cetirizine Dihydrochloride

[中文别名 ]:

[英文别名 ]:

Zirtek
EINECS 222-225-5
MFCD00941428
Zyrlex
cetirizine dihydrochloride
Cetirizine (dihydrochloride)

盐酸西替利嗪生物活性

[ 描述 ]:

Cetirizine二盐酸盐是第二代抗组胺剂,是hydroxyzine的主要代谢产物,是外消旋的选择性H1受体反向激动剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

[参考文献]

[1]. Naclerio RM. Additional properties of cetirizine, a new H1 antagonist. Allergy Proc. 1991 May-Jun;12(3):187-91.

[2]. Meh A, et al. Effect of cetirizine, a histamine (H(1)) receptor antagonist, on bone modeling during orthodontic tooth movement in rats. Am J Orthod Dentofacial Orthop. 2011 Apr;139(4):e323-9.

[相关活性小分子]

盐酸西替利嗪物理化学性质

[ 密度 ]:
1.237 g/cm3

[ 沸点 ]:
542.1ºC at 760 mmHg

[ 熔点 ]:
110-115ºC

[ 分子式 ]:
C₂₁H₂₇Cl₃N₂O₃

[ 分子量 ]:
461.81

[ 闪点 ]:
281.6ºC

[ PSA ]:
53.01000

[ LogP ]:
3.82600

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 储存条件 ]:
Desiccate at RT

盐酸西替利嗪MSDS

盐酸西替利嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AG0980000

CHEMICAL NAME :: Acetic acid, (2-(4-((4-chlorophenyl)phenylmethyl)-1-piperazinyl)et hoxy)-, dihydrochloride

CAS REGISTRY NUMBER :: 83881-52-1

LAST UPDATED :: 199606

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C21-H25-Cl-N2-O3.2Cl-H

MOLECULAR WEIGHT :: 461.85

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 365 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,1859,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 138 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4525358

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >320 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,1859,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18550 mg/kg/53W-I

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in thyroid weight Blood - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,1865,1994 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4680 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,1887,1994

盐酸西替利嗪安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
UN 3249

[ WGK德国 ]:
3

[ RTECS号 ]:
AG0977500

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933599090

盐酸西替利嗪合成路线

盐酸西替利嗪上下游产品

盐酸西替利嗪上游产品

盐酸西替利嗪下游产品

盐酸西替利嗪海关

[ 海关编码 ]: 2933599090

[ 中文概述 ]:
2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸西替利嗪文献

Involvement of the H1 Histamine Receptor, p38 MAP Kinase, Myosin Light Chains Kinase, and Rho/ROCK in Histamine-Induced Endothelial Barrier Dysfunction.

Microcirculation 22 , 237-48, (2015)

The mechanisms by which histamine increases microvascular permeability remain poorly understood. We tested the hypothesis that H1 receptor activation disrupts the endothelial barrier and investigated ...

Kinetics of the esterification of active pharmaceutical ingredients containing carboxylic acid functionality in polyethylene glycol: formulation implications.

J. Pharm. Sci. 103(8) , 2424-33, (2014)

Polyethylene glycols (PEGs) are attractive as excipients in the manufacture of drug products because they are water soluble and poorly immunogenic. They are used in various pharmaceutical preparations...

Histamine H4 and H1 receptors contribute to postinflammatory visceral hypersensitivity.

Gut 63(12) , 1873-82, (2014)

Substantial evidence implicates mast cells and their main constituent histamine in the pathogenesis of visceral hypersensitivity. We explored the specific contribution of histamine H4 (H4R) and H1 (H1...

更多文献

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盐酸西替利嗪-说明书-功效作用-盐酸西替利嗪片副作用

2019-01-06 16:43:53

导读：盐酸西替利嗪(Cetirizine)是一种抗过敏药，又称去敏定、司特宁、仙特明、协帝、CETIN或CETY，它是第二代H1抗组织胺药，为长效的具选择性的口服强效抗变态反应药。治疗过敏性鼻炎、由过敏原引起的荨麻疹及皮肤瘙痒有较好疗效。在中国，从2008年1月11日起，盐酸西替利嗪由处方药转换为...