产品说明书

Desloratadine

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Chemical Structure| 100643-71-8 同义名 : 脱羧氯雷他定 ;Sch34117;Descarboethoxyloratadine;Aerius;Neoclarityn;Clarinex;NSC 675447
CAS号 : 100643-71-8
货号 : A129917
分子式 : C19H19ClN2
纯度 : 98%
分子量 : 310.821
MDL号 : MFCD00871949
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(80.43 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：

4% DMSO+40% PEG 300+4% Tween 80+water 4 mg/mL

生物活性
靶点

  • H1 receptor

    Histamine H1 receptor, IC50:51 nM
描述 Desloratadine is a second-generation antihistamine for treatment of allergic disorders. At therapeutic doses, desloratadine did not bind significantly to brain H1Rs and did not induce any significant sedation[3]. Of the second-generation antihistamines, desloratadine has the greatest binding affinity for the H1 receptor. Desloratadine and fexofenadine do not impair cognitive or psychomotor functioning and are comparable with placebo in terms of somnolence[4]. Desloratadine is the orally active major metabolite of the nonsedating H1-antihistamine loratadine. Oral desloratadine 5 mg once daily for up to 4 weeks in patients with seasonal allergic rhinitis (SAR) significantly reduced nasal (including congestion) and non-nasal symptoms and improved health-related quality of life compared with placebo. Desloratadine 5 mg once daily for 6 weeks significantly improved pruritus and reduced the number of hives compared with placebo in patients with chronic idiopathic urticaria (CIU)[5].Desloratadine might have a negative effect on lactation in combination with a sympathomimetic agent such as pseudoephedrine[6]. Desloratadine treatment was also revealed to suppress colony-formation ability and induce cell cycle arrest at G1 phase in EJ cells. It promoted cell apoptosis via modulating the expression of Bcl-2, Bax, cleaved caspase 3, and cleaved caspase 9 in EJ and SW780 cells[7].
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
NCT00884325 - Completed - -
NCT03724240 Hay Fever Phase 3 Not yet recruiting December 2019 -
NCT03517930 Clinical Pharmacology Phase 1 Completed - United States, New Jersey ... 展开 >> Frontage Clinical Services Secaucus, New Jersey, United States, 07094 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.22mL

0.64mL

0.32mL

16.09mL

3.22mL

1.61mL

32.17mL

6.43mL

3.22mL
参考文献

[1]Geha RS, Meltzer EO. Desloratadine: A new, nonsedating, oral antihistamine. J Allergy Clin Immunol. 2001 Apr;107(4):751-62.

[2]Cardelus I, Anton F, et al. Anticholinergic effects of desloratadine, the major metabolite of loratadine, in rabbit and guinea-pig iris smooth muscle. Eur J Pharmacol. 1999 Jun 18;374(2):249-54.

[3]Nakamura T, Hiraoka K, Harada R, Matsuzawa T, Ishikawa Y, Funaki Y, Yoshikawa T, Tashiro M, Yanai K, Okamura N. Brain histamine H1 receptor occupancy after oral administration of desloratadine and loratadine. Pharmacol Res Perspect. 2019 Jul 12;7(4):e00499

[4]Devillier P, Roche N, Faisy C. Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30

[5]McClellan K, Jarvis B. Desloratadine. Drugs. 2001;61(6):789-96; discussion 797

[6]Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. Desloratadine. 2018 Oct 31

[7]Ma J, Qi J, Li S, Zhang C, Wang H, Shao L, Yuan X, Sha Q. Desloratadine, a Novel Antigrowth Reagent for Bladder Cancer. Technol Cancer Res Treat. 2020 Jan-Dec;19:1533033820926591