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氯雷他定 /Loratadine {[allProObj[0].p_purity_real_show]}

货号:A188364 同义名: Loratidine;SCH 29851

Loratadine is an inverse agonist of peripheral histamine H1-receptor with IC50 of > 32 μM.

Loratadine 化学结构 CAS号:79794-75-5
Loratadine 化学结构
CAS号:79794-75-5
Loratadine 3D分子结构
CAS号:79794-75-5
Loratadine 化学结构 CAS号:79794-75-5
Loratadine 3D分子结构 CAS号:79794-75-5
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Loratadine 纯度/质量文件 产品仅供科研

货号:A188364 标准纯度: {[allProObj[0].p_purity_real_show]}
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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 dihydrochloride 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 99%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
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

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
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。

Loratadine 生物活性

靶点
  • H1 receptor

    B(0)AT2, IC50:4 μM

描述 Loratadine, a selective inverse agonist of peripheral histamine H1-receptors, is a second-generation antihistaminic drugs suffers limited solubility, poor oral bioavailability (owing to extensive first-pass metabolism), and highly variable oral absorption[6]. Loratadine exerted its acute and chronic toxicity especially on Ceriodaphnia dubia (LC50: 600 µg/L, EC50: 28.14 µg/L)[3]. Loratadine at 0.5 and 5 mg/kg did not significantly affect the skeletal system of young rats. At 50 mg/kg, loratadine decreased the femoral length, increased content of calcium and phosphorus in the bone mineral of the vertebra, and tended to improve mechanical properties of the tibial metaphysis[4]. Loratadine is well tolerated. At dosages of 10 mg daily, commonly reported adverse events were somnolence, fatigue and headache. Sedation occurred less frequently with loratadine than with azatadine, cetirizine, chlorpheniramine, clemastine and mequitazine[5].

Loratadine 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
NCT01506791 Healthy Phase 1 Completed - United States, Florida ... 展开 >> SFBC Ft Myers Inc Broadway, Florida, United States, 33901 收起 <<
NCT00816972 Post-nasal Drip ... 展开 >> Seasonal Allergic Rhinitis Rhinorrhea 收起 << Phase 2 Completed - -
NCT00783211 Seasonal Allergic Rhinitis Phase 4 Completed - -

Loratadine 参考文献

[1]Delpon E, Valenzuela C, et al. Block of human cardiac Kv1.5 channels by loratadine: voltage-, time- and use-dependent block at concentrations above therapeutic levels. Cardiovasc Res. 1997 Aug;35(2):341-50.

[2]Genovese A, Patella V, et al. Loratadine and desethoxylcarbonyl-loratadine inhibit the immunological release of mediators from human Fc epsilon RI+ cells. Clin Exp Allergy. 1997 May;27(5):559-67.

[3]Iesce MR, Lavorgna M, Russo C, Piscitelli C, Passananti M, Temussi F, DellaGreca M, Cermola F, Isidori M. Ecotoxic effects of loratadine and its metabolic and light-induced derivatives. Ecotoxicol Environ Saf. 2019 Apr 15;170:664-672

[4]Folwarczna J, Konarek N, Freier K, Karbowniczek D, Londzin P, Janas A. Effects of loratadine, a histamine H1 receptor antagonist, on the skeletal system of young male rats. Drug Des Devel Ther. 2019 Sep 23;13:3357-3367

[5]Haria M, Fitton A, Peters DH. Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs. 1994 Oct;48(4):617-37

[6]Elkomy MH, El Menshawe SF, Abou-Taleb HA, Elkarmalawy MH. Loratadine bioavailability via buccal transferosomal gel: formulation, statistical optimization, in vitro/in vivo characterization, and pharmacokinetics in human volunteers. Drug Deliv. 2017 Nov;24(1):781-791

Loratadine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.06mL

2.61mL

1.31mL

26.12mL

5.22mL

2.61mL

Loratadine 技术信息

CAS号79794-75-5
分子式C22H23ClN2O2
分子量 382.883
别名 Loratidine;SCH 29851;Wyeth Brand of Loratadine;Loratadine Wyeth Brand;Alavert;Clarityn;Claritin
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Room Temperature

溶解度

DMSO: 50 mg/mL(130.59 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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