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Brompheniramine maleate

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Chemical Structure| 980-71-2 同义名 : (±)-Brompheniramine maleate;Brompheniramine (maleate);(±)-Brompheniramine;Brompheniramine hydrogen maleate
CAS号 : 980-71-2
货号 : A312159
分子式 : C20H23BrN2O4
纯度 : 98%
分子量 : 435.312
MDL号 : MFCD00057367
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(241.21 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

H2O: 100 mg/mL(229.72 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 40 mg/mL suspension

生物活性
靶点

  • H1 receptor
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 ... 展开 >> Moorabin Hospital Not yet recruiting Melbourne, Victoria, Australia, 8148 Contact: Alison Fitz-Gerald, MBBS    +61417 354 743    fitzali@gmail.com 收起 <<
NCT00894634 Allergic Reactions Not Applicable Completed - -
NCT01177852 Inflammation ... 展开 >>Cough Rhinitis 收起 << Phase 3 Withdrawn - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.49mL

2.30mL

1.15mL

22.97mL

4.59mL

2.30mL
参考文献

[1]Gwaltney JM Jr, Druce HM. Efficacy of brompheniramine maleate for the treatment of rhinovirus colds. Clin Infect Dis. 1997 Nov;25(5):1188-94.

[2]Cox DC, Kirchhoefer RD. Semiautomated method for the analysis of formulations of chlorpheniramine maleate and brompheniramine maleate. J Assoc Off Anal Chem. 1979 May;62(3):552-5.

[3]Chiu CC, Chen JY, Chen YW, Wang JJ, Hung CH. Subcutaneous brompheniramine for cutaneous analgesia in rats. Eur J Pharmacol. 2019 Oct 5;860:172544

[4]Thoden WR, Druce HM, Furey SA, Lockhart EA, Ratner P, Hampel FC, van Bavel J. Brompheniramine maleate: a double-blind, placebo-controlled comparison with terfenadine for symptoms of allergic rhinitis. Am J Rhinol. 1998 Jul-Aug;12(4):293-9

[5]Gwaltney JM Jr, Druce HM. Efficacy of brompheniramine maleate for the treatment of rhinovirus colds. Clin Infect Dis. 1997 Nov;25(5):1188-94

[6]Ormerod AD, Baker R, Watt J, White MI. Terfenadine and brompheniramine maleate in urticaria and dermographism. Dermatologica. 1986;173(1):5-8