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/ Cetirizine 2HCl/盐酸西替利嗪

Cetirizine 2HCl/盐酸西替利嗪 {[allProObj[0].p_purity_real_show]}

货号：A535405 同义名： P071; Cetirizine (hydrochloride)

Cetirizine 2HCl 是羟嗪的代谢产物，作为 H₁ 受体的选择性反向激动剂，常用于过敏、花粉症及荨麻疹的研究。

Cetirizine 2HCl/盐酸西替利嗪 化学结构 CAS号：83881-52-1
Cetirizine 2HCl/盐酸西替利嗪 化学结构
CAS号：83881-52-1
Cetirizine 2HCl/盐酸西替利嗪 3D分子结构
CAS号：83881-52-1
Cetirizine 2HCl/盐酸西替利嗪 化学结构 CAS号：83881-52-1
Cetirizine 2HCl/盐酸西替利嗪 3D分子结构 CAS号：83881-52-1
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Cetirizine 2HCl/盐酸西替利嗪 纯度/质量文件 产品仅供科研

货号：A535405 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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更多 >
产品名称 H1 receptor ↓ H2 receptor ↓ H3 receptor ↓ H4 receptor ↓ Histamine receptor ↓ 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine ✔ 97%
Loratadine +

B(0)AT2, IC50: 4 μM

 		98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

 		98%
Doxylamine succinate ✔ 99%
Ebastine ✔ 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

 		98%
Meclizine 2HCl ✔ 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

 		99%
Diphenhydramine HCl ✔ 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

 		++

H2 receptor, pKi: 7.2

 		99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

 		99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

 		98%
Pemirolast potassium ✔ 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

 		98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

 		98%
Brompheniramine maleate ✔ 98%
Carbinoxamine maleate salt ✔ 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

 		98%
Ketotifen fumarate salt ✔ 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

 		PAFR 98%
Famotidine ✔ 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

 		98%
Lafutidine ✔ 99%
Cimetidine ✔ 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

 		AChE 98%
Ranitidine ✔ 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

 		99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

 		99%+
S 38093 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 μM

 		98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

 		99%
Azelastine HCl ✔ 98%
Epinastine HCl ✔ 99%
Levodropropizine ✔ 97%
Cyproheptadine HCl ✔ 98%
Hesperetin ✔ 97%
Olopatadine HCl ✔ 98%
Mianserin HCl ✔ 99+%
Buclizine 2HCl ✔ 95%
Latrepirdine 2HCl ✔ GluR 99%
Cetirizine 2HCl ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cetirizine 2HCl/盐酸西替利嗪 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].

Cetirizine 2HCl/盐酸西替利嗪 细胞实验

Cell Line
Concentration Treated Time Description References
Murine eosinophils cultured from bone marrow 5 μM 30 minutes To measure the inhibitory effect of cetirizine on eosinophil degranulation, results showed cetirizine significantly reduced EPO release. J Clin Invest. 2013;123(5):2306-2316.
Guinea-pig ventricular myocytes 0.1 μM 10 minutes Cetirizine at 0.1 μM reduced IKr to 49%, while IKs was only inhibited to 79%. Br J Pharmacol. 1998 Jun;124(4):663-8.
Rabbit ventricular myocytes 0.1 μM 10 minutes To analyze the effect of cetirizine on delayed K+ currents, results showed cetirizine inhibited IKr current with an IC50 of 108 μM. Br J Pharmacol. 1998 Jun;124(4):663-8.

Cetirizine 2HCl/盐酸西替利嗪 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice NMO model Oral 10 mg/kg Twice daily for 3 days To study the inhibitory effect of cetirizine on NMO lesions, results showed cetirizine significantly reduced lesion severity and eosinophil infiltration. J Clin Invest. 2013;123(5):2306-2316.
Balb/C mice Ovalbumin-sensitized peritonitis model Subcutaneous injection 15-30 mg/kg 1 hour before and 6 hours after Cetirizine significantly reduced ovalbumin-induced eosinophil accumulation, whereas terfenadine was ineffective, suggesting that the effect of cetirizine was not related to the inhibition of the H1 receptor effects of histamine. Br J Pharmacol. 1993 Oct;110(2):917-24
Male Wistar rats PAF or compound 48/80-induced pleural eosinophil accumulation model Intraperitoneal or intrathoracic 5 to 30 mg/kg (i.p.) or 5 and 15 μg/cavity (i.t.) Single dose, 1 h before (i.p.) or 5 min before (i.t.) To evaluate the inhibitory effect of cetirizine on PAF or compound 48/80-induced pleural eosinophil accumulation, results showed that cetirizine significantly inhibited eosinophil accumulation, and this effect was not related to its antagonism of histamine H1 receptors. Br J Pharmacol. 1992 Jan;105(1):176-80.
Guinea-pigs Ovalbumin-sensitized paw oedema model Subcutaneous injection 20 mg/kg Single dose, measured 30 minutes after administration To evaluate the inhibitory effect of cetirizine on ovalbumin-induced paw oedema, results showed cetirizine was ineffective Br J Pharmacol. 1994 May;112(1):111-6
C57BL/6J male mice DMM-induced osteoarthritis model Oral gavage 100μg/day Once daily for 12 weeks To evaluate the effect of cetirizine on the development of osteoarthritis in the DMM mouse model. Results showed that cetirizine significantly attenuated cartilage degeneration and reduced the expression of OA-related mediator genes. Clin Immunol. 2022 Nov;244:109117
DBA/2 mice Viral myocarditis model Oral 1 or 10 mg/kg/day Once daily, starting on the day of viral inoculation Cetirizine improved survival dose dependently, significantly decreased the heart weight to body weight ratio, reduced the area of myocardial necrosis, and suppressed the gene expressions of tumor necrosis factor, interleukin 6, and metalloproteinase 2. J Inflamm (Lond). 2010 Aug 4;7:39
Guinea pigs Non-immunized guinea pigs receiving platelets from immunized animals Intravenous injection 10-30 mg/kg Administered 1 hour before antigen challenge Cetirizine dose-dependently inhibited platelet-dependent leucopenia, with the highest dose achieving complete inhibition. Terfenadine and mepyramine were ineffective. Br J Pharmacol. 1991 Jun;103(2):1520-4

Cetirizine 2HCl/盐酸西替利嗪 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 - -

Cetirizine 2HCl/盐酸西替利嗪 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

Cetirizine 2HCl/盐酸西替利嗪 实验方案

计算器
存储液制备 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

Cetirizine 2HCl/盐酸西替利嗪 技术信息

CAS号83881-52-1
分子式C21H27Cl3N2O3
分子量 461.81
SMILES Code O=C(COCCN1CCN(CC1)C(C2=CC=CC=C2)C3=CC=C(Cl)C=C3)O.[H]Cl.[H]Cl
MDL No. MFCD00941428
别名 P071; Cetirizine (hydrochloride); UCB-P 071; Cetirizine DiHCl; Cetirizine dihydrochloride
运输蓝冰
InChI Key PGLIUCLTXOYQMV-UHFFFAOYSA-N
Pubchem ID 55182
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Cetirizine | 83881-52-1 | P071 | P 071 | P-071 | H1-receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Cetirizine 2HCl/盐酸西替利嗪 纯度/质量文件 | Cetirizine 2HCl/盐酸西替利嗪 亚型比较 | Cetirizine 2HCl/盐酸西替利嗪 生物活性 | Cetirizine 2HCl/盐酸西替利嗪 临床数据 | Cetirizine 2HCl/盐酸西替利嗪 参考文献 | Cetirizine 2HCl/盐酸西替利嗪 实验方案 | Cetirizine 2HCl/盐酸西替利嗪 技术信息

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