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CAS No.: 980-71-2

Brompheniramine maleate/马来酸溴苯那敏 Catalog No. CSN10492

Synonyms: (±)-Brompheniramine maleate;Brompheniramine Hydrogen Maleate;Brompheniramine (maleate)

Brompheniramine maleate is an antagonist of histamine H1 receptors.

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技术信息

生物活性

描述Brompheniramine maleate is a potent and orally active antihistamine of the propylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate has anticholinergic, antidepressant and analgesia properties and can be used for allergic rhinitis research. Brompheniramine as an antihistamine blocks sodium channels. Brompheniramine (3.0, 1.5, 1.1, 0.6, and 0.3 μmol) treatment shows cutaneous analgesic effect with an ED50 value of 0.89 μmol in a rat model of infiltration anesthesia. Subcutaneous Brompheniramine induces dose-relatedly analgesic effects, and Brompheniramine induces prolonged analgesic duration. In vitro, Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells, sodium and calcium channels in CHO cells, as well as potassium channels in human embryonic kidney 293 (HEK-293) cells. Brompheniramine suppresses the transfected Nav1.5 channels from myocytes^[3]. An extended-release formulation of brompheniramine 12 mg or 8 mg bid alleviates allergic rhinitis symptoms and brompheniramine 12 mg provides significantly better relief of these symptoms than terfenadine 60 mg bid^[4]. Treatment with brompheniramine was associated with the adverse effects of somnolence (n = 3) and confusion (n = 1). Brompheniramine was efficacious treatment for the sneezing, rhinorrhea, and cough associated with rhinovirus colds^[5]. Brompheniramine maleate was more effective than terfenadine in the patients with dermographism^[6].
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
NCT00456170	Vaginal Hysterectomy	Phase 1	Unknown	-	Australia, Victoria ... more >> Moorabin Hospital Not yet recruiting Melbourne, Victoria, Australia, 8148 Contact: Alison Fitz-Gerald, MBBS +61417 354 743 fitzali@gmail.com Collapse <<
NCT00894634	Allergic Reactions	Not Applicable	Completed	-	-
NCT01177852	Inflammation ... more >>Cough Rhinitis Collapse <<	Phase 3	Withdrawn	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2972 mL
- 11.4860 mL
- 22.9721 mL
- 5 mM
- 0.4594 mL
- 2.2972 mL
- 4.5944 mL
- 10 mM
- 0.2297 mL
- 1.1486 mL
- 2.2972 mL

技术信息

CAS号

980-71-2

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H23BrN2O4

运输

蓝冰

分子量

435.31

别名

(±)-Brompheniramine maleate;Brompheniramine Hydrogen Maleate;Brompheniramine (maleate);(±)-Brompheniramine;Brompheniramine;Bromfed;Dimetapp;Bromfenex;Dimetane;BPN;Lodrane;马来酸溴苯那敏

溶解度

DMSO	410.0 mg/mL (941.9 mM) warming
Water	80.0 mg/mL (183.8 mM) warming

动物实验配方

0.5% CMC-Na

40 mg/mL

suspension

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Brompheniramine maleate/马来酸溴苯那敏 Catalog No. CSN10492

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