Description
Brompheniramine is a halogenated antihistamine derivative of pheniramine that exhibits anticholinergic and neuromodulatory activities. Brompheniramine inhibits the H1 histamine receptor and also displays non-selective inhibition of muscarinic acetylcholine receptors (mAChRs). Brompheniramine inhibits histamine-induced vasodilation and also potentiates the effects of opioid analgesics. Additionally, brompheniramine is the parent compound of zimelidine, a selective serotonin reuptake inhibitor (SSRI) that exhibits antidepressant activity; zimelidine inhibits pre-synaptic 5-HT reuptake and may inhibit the serotonin transporter (SERT) or monoamine oxidase B (MAO-B).
References
Egashira T, Takayama F, Yamanaka Y. The inhibition of monoamine oxidase activity by various antidepressants: differences found in various mammalian species. Jpn J Pharmacol. 1999 Sep;81(1):115-21. PMID: 10580379.
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. PMID: 10212017.
Tatsumi M, Groshan K, Blakely RD, et al. Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. PMID: 9537821.
Dachman WD, Bedarida G, Blaschke TF, et al. Histamine-induced venodilation in human beings involves both H1 and H2 receptor subtypes. J Allergy Clin Immunol. 1994 Mar;93(3):606-14. PMID: 8151062.
Ogren SO, Ross SB, Hall H, et al. The pharmacology of zimelidine: a 5-HT selective reuptake inhibitor. Acta Psychiatr Scand Suppl. 1981;290:127-51. PMID: 6452789.
