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/ 组胺受体 / Chlorpheniramine maleate

马来酸氯苯那敏 /Chlorpheniramine maleate {[allProObj[0].p_purity_real_show]}

货号：A352417 同义名： Chlorphenamine maleate;Chlorpheniramine (maleate)

Chlorpheniramine maleate is an antagonist of histamine H1 receptor with IC50 of 12 nM.

Chlorpheniramine maleate 化学结构 CAS号：113-92-8
Chlorpheniramine maleate 化学结构
CAS号：113-92-8
Chlorpheniramine maleate 3D分子结构
CAS号：113-92-8
Chlorpheniramine maleate 化学结构 CAS号：113-92-8
Chlorpheniramine maleate 3D分子结构 CAS号：113-92-8
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Chlorpheniramine maleate 纯度/质量文件 产品仅供科研

货号：A352417 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

Chlorpheniramine maleate 生物活性

靶点

  • H1 receptor

    Histamine H1 receptor, IC50:12 nM
描述 Chlorpheniramine Maleate is potent, less sedative antihistaminic drug, which acts by inhibiting histamine release from mast cells. Chlorpheniramine causes bronchodilation during resting period by acting on the circulating or tissue histamine in asthmatics which contributes to an increase in resting bronchomotor tone[3]. Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds. Age, dialysis, urinary pH and flow influence the elimination kinetics of chlorpheniramine[4]. A nasal gel formulation for an antihistaminic drug, Chlorpheniramine maleate (CPM), which suffers from poor oral[5]. The antihistamine chlorpheniramine maleate (CPM) is also used for symptomatic relief of hypersensitive reactions and in pruritic skin disorders[6].

Chlorpheniramine maleate 参考文献

[1]Medina MA, Garcia de Veas R, et al. Chlorpheniramine inhibits the synthesis of ornithine decarboxylase and the proliferation of human breast cancer cell lines. Breast Cancer Res Treat. 1995 Aug;35(2):187-94.

[2]Sleevi MC, Cale AD Jr, et al. Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines. J Med Chem. 1991 Apr;34(4):1314-28.

[3]Chugh J, Yadav YR, Kulkarni HS, Maheshwari S. The Effect of Aerosolized Chlorpheniramine Maleate on Exercise Induced Bronchospasm and Gas Exchange in Asthmatics. J Assoc Physicians India. 2020 Apr;68(4):21-25

[4]Rumore MM. Clinical pharmacokinetics of chlorpheniramine. Drug Intell Clin Pharm. 1984 Sep;18(9):701-7

[5]Soliman II, Soliman NA, Abdou EM. Formulation and stability study of chlorpheniramine maleate nasal gel. Pharm Dev Technol. 2010 Sep-Oct;15(5):484-91

[6]Ceschel GC, Maffei P, Gentile M. Design and evaluation of a new transdermal formulation containing chlorpheniramine maleate. Drug Dev Ind Pharm. 1999 Sep;25(9):1035-9

Chlorpheniramine maleate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.79mL

2.56mL

1.28mL

25.58mL

5.12mL

2.56mL

Chlorpheniramine maleate 技术信息

CAS号113-92-8
分子式C20H23ClN2O4
分子量 390.86
别名 Chlorphenamine maleate;Chlorpheniramine (maleate);Chlor-100;Chlo-Amine;Bayer Brand of Chlorpheniramine Maleate;Neorestamin;Deconamine;Chlortrimeton;Piriton;Chlorprophenpyridamine;(±)-Chlorpheniramine;NCI-C55265
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,Room temperature
溶解度

DMSO: 105 mg/mL(268.64 mM)，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

H2O: 30 mg/mL(76.75 mM)，配合低频超声助溶
动物实验配方

Tags: Chlorpheniramine maleate |马来酸氯苯那敏 | Chlorphenamine maleate | Chlorpheniramine (maleate) | Chlor-100 | Chlo-Amine | Bayer Brand of Chlorpheniramine Maleate | Neorestamin | Deconamine | Chlortrimeton | Piriton | Chlorprophenpyridamine | (±)-Chlorpheniramine | NCI-C55265 | 113-92-8 | 组胺受体 | Chlorpheniramine maleate 纯度/质量文件 | Chlorpheniramine maleate 亚型比较 | Chlorpheniramine maleate 生物活性 | Chlorpheniramine maleate 参考文献 | Chlorpheniramine maleate 实验方案 | Chlorpheniramine maleate 技术信息

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