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

货号:A129917 同义名: 脱羧氯雷他定 / Sch34117;Descarboethoxyloratadine

Desloratadine is an antagonist of histamine H1 receptor that is used to treat allergies.

Desloratadine 化学结构 CAS号:100643-71-8
Desloratadine 化学结构
CAS号:100643-71-8
Desloratadine 3D分子结构
CAS号:100643-71-8
Desloratadine 化学结构 CAS号:100643-71-8
Desloratadine 3D分子结构 CAS号:100643-71-8
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Desloratadine 纯度/质量文件 产品仅供科研

货号:A129917 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 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 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。

Desloratadine 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].

Desloratadine 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 <<

Desloratadine 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

Desloratadine 实验方案

计算器
存储液制备 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

Desloratadine 技术信息

CAS号100643-71-8
分子式C19H19ClN2
分子量 310.821
别名 脱羧氯雷他定 ;Sch34117;Descarboethoxyloratadine;Aerius;Neoclarityn;Clarinex;NSC 675447
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,Inert atmosphere,2-8°C

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

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