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/ 组胺受体 / Brompheniramine maleate

马来酸溴苯那敏 /Brompheniramine maleate {[allProObj[0].p_purity_real_show]}

货号：A312159 同义名： (±)-Brompheniramine maleate;Brompheniramine (maleate)

Brompheniramine maleate is an antagonist of histamine H1 receptors.

Brompheniramine maleate 化学结构 CAS号：980-71-2
Brompheniramine maleate 化学结构
CAS号：980-71-2
Brompheniramine maleate 3D分子结构
CAS号：980-71-2
Brompheniramine maleate 化学结构 CAS号：980-71-2
Brompheniramine maleate 3D分子结构 CAS号：980-71-2
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Brompheniramine maleate 纯度/质量文件 产品仅供科研

货号：A312159 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 ✔ 98%
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。

Brompheniramine maleate 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].

Brompheniramine maleate 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 - -

Brompheniramine maleate 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

Brompheniramine maleate 实验方案

计算器
存储液制备 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

Brompheniramine maleate 技术信息

CAS号980-71-2
分子式C20H23BrN2O4
分子量 435.312
别名 (±)-Brompheniramine maleate;Brompheniramine (maleate);(±)-Brompheniramine;Brompheniramine hydrogen maleate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
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

Tags: Brompheniramine | 980-71-2 | (±)-Brompheniramine | Histamine Receptor | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Membrane Transporter/Ion Channel | Histamine Receptor | mAChR | Potassium Channel | Sodium Channel | Calcium Channel | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Brompheniramine maleate 纯度/质量文件 | Brompheniramine maleate 亚型比较 | Brompheniramine maleate 生物活性 | Brompheniramine maleate 临床数据 | Brompheniramine maleate 参考文献 | Brompheniramine maleate 实验方案 | Brompheniramine maleate 技术信息

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