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].
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