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Brompheniramine

Catalog No. T60843   CAS 86-22-6

Brompheniramine ((±)-Brompheniramine) is a potent and orally active alkylamine class antihistamine. Brompheniramine is a selective antagonist of histamine H1 receptor (Kd = 6.06 nM). Brompheniramine can be used in the research of allergic rhinitis that has anticholinergic, antidepressant and anesthetic properties. Brompheniramine can block the calcium channels, sodium channels, and hERG channels with IC 50 s of 16.12 μM, 21.26 μM, and 0.90 μM, respectively [1] [2] [3] [4].

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Brompheniramine Chemical Structure
Brompheniramine, CAS 86-22-6
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25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
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Description Brompheniramine ((±)-Brompheniramine) is a potent and orally active alkylamine class antihistamine. Brompheniramine is a selective antagonist of histamine H1 receptor (Kd = 6.06 nM). Brompheniramine can be used in the research of allergic rhinitis that has anticholinergic, antidepressant and anesthetic properties. Brompheniramine can block the calcium channels, sodium channels, and hERG channels with IC 50 s of 16.12 μM, 21.26 μM, and 0.90 μM, respectively [1] [2] [3] [4].
In vitro Brompheniramine, at concentrations ranging from 0.1-100 μM, inhibits hERG K+ channels in CHO cells in a concentration-dependent manner, with an IC50 value of 0.90±0.14 μM. This effect is observed through the reduction of peak tail current amplitude at -60 mV, following a depolarization-repolarization protocol [3]. Additionally, brompheniramine at 1, 10, and 100 μM concentrations significantly shortens the APD50 and depresses the plateau phase of the action potential in guinea pig papillary muscle, while at 10 and 100 μM, it slightly prolongs the APD90 [3]. Furthermore, brompheniramine reduces the amplitude of 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]. The compound also blocks muscarinic cholinergic receptors in human CHO cells [4].
In vivo Brompheniramine (0.3-3 μM; SC, single dosage) elicits dose-dependent cutaneous analgesia in male Sprague-Dawley rats [1]. Administered via a single subcutaneous injection in doses ranging from 0.3 to 3.0 μM, it resulted in cutaneous analgesia with an effective concentration (EC 50) of 0.66 μM, alongside an extended duration of analgesia.
Molecular Weight 319.24
Formula C16H19BrN2
CAS No. 86-22-6

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