Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selectivehistamine H1 receptorantagonist with aK_dof 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].

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].

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

319.24

C₁₆H₁₉BrN₂

86-22-6

溴苯那敏

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