Drug intelligence / Profile preview

diphenhydramine

Development stage
Approved
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral, Topical, Intravenous, Intramuscular
01

Overview

Diphenhydramine is a first-generation antihistamine and sedative primarily used to treat symptoms of allergies (such as sneezing, runny nose, itchy or watery eyes), the common cold, motion sickness, insomnia, and certain symptoms of Parkinson's disease. It acts mainly as an inverse agonist at the histamine H1 receptor and also has significant anticholinergic properties. By blocking H1 receptors on effector cells in various tissues (including respiratory smooth muscle and vascular endothelium), it prevents but does not reverse histamine-mediated responses such as increased vascular permeability and sensory nerve stimulation. Its antiemetic effects are mediated through inhibition at the medullary chemoreceptor trigger zone. Diphenhydramine was developed by George Rieveschl and introduced commercially in 1946[4][5][6].

Brand names
BenadrylAllergy ReliefAllermaxBanophenCompoz Nighttime Sleep Aid
Other names
diphenhydramine
02

Targets

SERT (Sodium-dependent serotonin transporter)M1 (Muscarinic acetylcholine receptor M1)HRH1 (Histamine H1 Receptor)KCNH2 (Voltage-gated potassium channel subfamily H member 2)CHRM4 (M4)DRD2 (Dopamine D2 Receptor)CHRM3 (M3)CHRM5 (M5)CHRM2 (M2)NET (Norepinephrine Transporter)

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