brompheniramine

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[1][2][3][4].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Endocrinology

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

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].

Brompheniramine (0.3-3 μM; SC, single dosage) induces cutaneous analgesia in rats[1]. Animal Model: Male Sprague-Dawley rats[1] 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.

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

[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.

[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.

[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.