产品说明书

Loratadine

Print
Chemical Structure| 79794-75-5 同义名 : Loratidine;SCH 29851;Wyeth Brand of Loratadine;Loratadine Wyeth Brand;Alavert;Clarityn;Claritin
CAS号 : 79794-75-5
货号 : A188364
分子式 : C22H23ClN2O2
纯度 : 98%
分子量 : 382.883
MDL号 : -
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 - -
实验方案
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
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