Brompheniramine  (Synonyms: (±)-Brompheniramine)

Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a K_d 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^[1][2][3][4].

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)^[3].
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^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

319.24

C₁₆H₁₉BrN₂

86-22-6

Liquid

Colorless to light yellow

CN(C)CCC(C1=CC=C(Br)C=C1)C2=CC=CC=N2

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Chong-Chi Chiu, et al. Subcutaneous brompheniramine for cutaneous analgesia in rats. Eur J Pharmacol. 2019 Oct 5;860:172544.  [Content Brief]

  [2]. B Cusack, et al. Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65.  [Content Brief]

  [3]. Shin WH, Kim KS, Kim EJ. Electrophysiological effects of brompheniramine on cardiac ion channels and action potential. Pharmacol Res. 2006 Dec;54(6):414-20.  [Content Brief]

  [4]. Yasuda SU, Yasuda RP. Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51.  [Content Brief]