产品说明书

Cetirizine 2HCl

Print
Chemical Structure| 83881-52-1 同义名 : P071;Cetirizine (hydrochloride);UCB-P 071;Cetirizine DiHCl;Cetirizine dihydrochloride
CAS号 : 83881-52-1
货号 : A535405
分子式 : C21H27Cl3N2O3
纯度 : 98%
分子量 : 461.81
MDL号 : MFCD00941428
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Histamine receptor
描述 Cetirizine dihydrochloride, a second-generation antihistamine and a human metabolite of hydroxyzine, is an orally-active and selective histamine H1-receptor antagonist[3]. Cetirizine exhibits high intestinal absorption in humans and its oral bioavailability is estimated to be greater than 70%[4]. Compared with the majority of other SGAHs (second-generation H1 antihistamines), cetirizine was generally shown to have a more favourable pharmacological profile, to be well tolerated, be at least equally or more efficacious in attenuating/inhibiting nasal and ocular symptoms and to improve the quality of life in AR ((allergic rhinitis) patients[5]. Cetirizine may also have a role in the treatment of certain forms of physical urticaria, atopic dermatitis and reactions to mosquito bites[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00628108 Allergic Rhinitis ... 展开 >> Chronic Urticaria 收起 << Phase 3 Completed - United States, Alabama ... 展开 >> Birmingham, Alabama, United States United States, Arkansas Hot Springs, Arkansas, United States Jonesboro, Arkansas, United States Little Rock, Arkansas, United States United States, California Bakersfield, California, United States Crescent City, California, United States Huntington Beach, California, United States Los Angeles, California, United States Orange, California, United States Roseville, California, United States Stockton, California, United States United States, Georgia Albany, Georgia, United States Gainesville, Georgia, United States United States, Illinois Normal, Illinois, United States United States, Missouri Bridgeton, Missouri, United States United States, Nebraska Omaha, Nebraska, United States United States, Oklahoma Oklahoma City, Oklahoma, United States United States, South Carolina Barnwell, South Carolina, United States Spartanburg, South Carolina, United States United States, Tennessee Kingsport, Tennessee, United States United States, Texas Austin, Texas, United States Dallas, Texas, United States El Paso, Texas, United States San Antonio, Texas, United States Sugarland, Texas, United States United States, Virginia Richmond, Virginia, United States 收起 <<
NCT00521131 Rhinitis Alle... 展开 >>rgic Perennial 收起 << Phase 4 Completed - -
NCT00520754 Cough Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.65mL

4.33mL

2.17mL
参考文献

[1]Meh A, Sprogar S, 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.

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

[3]Portnoy JM, Dinakar C. Review of cetirizine hydrochloride for the treatment of allergic disorders. Expert Opin Pharmacother. 2004 Jan;5(1):125-35

[4]Chen C. Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine. Curr Med Chem. 2008;15(21):2173-91

[5]Zhang L, Cheng L, Hong J. The clinical use of cetirizine in the treatment of allergic rhinitis. Pharmacology. 2013;92(1-2):14-25

[6]Spencer CM, Faulds D, Peters DH. Cetirizine. A reappraisal of its pharmacological properties and therapeutic use in selected allergic disorders. Drugs. 1993 Dec;46(6):1055-80