The Sound of Evolution
Chlorpheniramine
Mechanism of action:
Chlorpheniramine is a first-generation H₁ receptor antagonist of the alkylamine class. Chlorpheniramine binds to H₁ receptors in both the peripheral and central nervous systems and blocks histamine from binding to them. This prevents typical allergic responses such as vasodilation, increased capillary permeability, smooth muscle contraction, and sensory nerve stimulation. Chlorpheniramine suppresses these effects.
Reference(s):
1. Chen X et al. (2002). TTD: Therapeutic Target Database. Nucleic Acids Res.
2. Tagawa M et al. (2001). Neuroimaging of histamine H1-receptor occupancy in human brain by positron emission tomography (PET): a comparative study of ebastine, a second-generation antihistamine, and (+)-chlorpheniramine, a classical antihistamine. Br J Clin Pharmacol.