Description
Diphenhydramine is a first generation antihistamine that exhibits anti-tussive, antiemetic, sedative, anti-allergic, and anticholinergic activities. Diphenhydramine inhibits muscarinic acetylcholine receptors (mAChRs) and Na+ channels and acts as an inverse agonist at histamine H1 receptors. In vivo, diphenhydramine decreases leukocyte infiltration into injury sites.
References
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Kim YS, Shin YK, Lee C, et al. Block of sodium currents in rat dorsal root ganglion neurons by diphenhydramine. Brain Res. 2000 Oct 27;881(2):190-8. PMID: 11036158.
Reiner PB, Kamondi A. Mechanisms of antihistamine-induced sedation in the human brain: H1 receptor activation reduces a background leakage potassium current. Neuroscience. 1994 Apr;59(3):579-88. PMID: 8008209.