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Brompheniramine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Brompheniramine图片
CAS NO:86-22-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
溴苯那敏
(±)-Brompheniramine
产品介绍
Brompheniramine ((±)-Brompheniramine) 是一种有效的口服有效的烷基胺类抗组胺药。Brompheniramine 是一种选择性组胺 H1 受体 (histamine H1 receptor) 拮抗剂,Kd为 6.06 nM。Brompheniramine 可阻断 hERG 通道 (hERG channels)、钙离子通道 (calcium channels) 和钠离子通道 (sodium channels),IC50分别为 0.90 μM、16.12 μM 和 21.26 μM。Brompheniramine 具有抗胆碱能、抗抑郁以及麻醉作用,可用于过敏性鼻炎和缓解疼痛的研究。
生物活性

Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selectivehistamine H1 receptorantagonist with aKdof 6.06 nM. Brompheniramine can block thehERG channels,calcium channels, andsodium channelswithIC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].

体外研究
(In Vitro)

Brompheniramine (0.1-100 μM) blocks hERG K+channels expressed in CHO cells in a concentration-dependent manner with an IC50of 0.90±0.14 μM, and reduced peak tail current amplitude measured at -60 mV (cells are depolarized for 2 s to +20 mV from a holding potential of -80 mV followed by a 3s repolarization back to -60 mV)[3].
Brompheniramine (1, 10 and 100 μM) significantly shortens the APD50and depresses the plateau phase on the action potential in guinea pig papillary muscle, as well as slightly prolongs the APD90in guinea pig papillary muscle at 10 and 100 μM[3].
Brompheniramine (0.1-100 μM) inhibit the amplitude of the Ca2+channel currents in rat ventricular myocytes by 14.1±1.1, 31.1±5.8, 38.0±3.8 and 90.2±3.7% at 0.1, 1, 10 and 100 μM, respectively[3].
Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells[4].

体内研究
(In Vivo)

Brompheniramine (0.3-3 μM; SC, single dosage) induces cutaneous analgesia in rats[1].

Animal Model:Male Sprague-Dawley rats[1]
Dosage:0.3, 0.6, 1.1, 1.5 and 3.0 μM
Administration:SC, single dosage
Result:Provoked cutaneous analgesia in a dose-dependent manner, with an EC50value of 0.66 μM, and induced prolonged analgesic duration.
Clinical Trial
分子量

319.24

Formula

C16H19BrN2

CAS 号

86-22-6

中文名称

溴苯那敏

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.