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编 号：F485220
分子式：C16H19BrN2
分子量：319.24
分子式：C16H19BrN2
分子量：319.24
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CAS No: 86-22-6
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生物活性：
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s 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.
体内研究：
Brompheniramine (0.3-3?μM; SC, single dosage) induces cutaneous analgesia in rats.Animal Model:Male Sprague-Dawley rats
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 EC50 value of 0.66 μM, and induced prolonged analgesic duration.
体外研究：
Brompheniramine (0.1-100 μM) blocks hERG K+ channels expressed in CHO cells in a concentration-dependent manner with an IC50 of 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).Brompheniramine (1, 10 and 100 μM) significantly shortens the APD50 and depresses the plateau phase on the action potential in guinea pig papillary muscle, as well as slightly prolongs the APD90 in guinea pig papillary muscle at 10 and 100 μM.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.Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells.
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s 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.
体内研究：
Brompheniramine (0.3-3?μM; SC, single dosage) induces cutaneous analgesia in rats.Animal Model:Male Sprague-Dawley rats
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 EC50 value of 0.66 μM, and induced prolonged analgesic duration.
体外研究：
Brompheniramine (0.1-100 μM) blocks hERG K+ channels expressed in CHO cells in a concentration-dependent manner with an IC50 of 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).Brompheniramine (1, 10 and 100 μM) significantly shortens the APD50 and depresses the plateau phase on the action potential in guinea pig papillary muscle, as well as slightly prolongs the APD90 in guinea pig papillary muscle at 10 and 100 μM.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.Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells.
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