Drug intelligence / Profile preview

aprofene

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

Aprofene (also known as aprophen or aprophene) is a synthetic small molecule drug developed in the Soviet Union that functions as an antagonist of both muscarinic and nicotinic acetylcholine receptors. It acts as a noncompetitive inhibitor at the nicotinic acetylcholine receptor, particularly binding to the desensitized state of the receptor and blocking ion flow without directly competing at the agonist (orthosteric) site[9][7]. Historically, aprofene has been used mainly in Russia for the treatment of endarteritis (inflammation of arterial intima), peptic ulcers, cholecystitis (gallbladder inflammation), and spastic colitis. It also has anticholinergic properties affecting both the central and peripheral nervous systems. Its use appears largely historical or regional, as it is not widely registered or marketed outside Russia and former Soviet countries[5][9][1].

Brand names
aprophene
Other names
aprofeneaprophenAprofenumAprofenoalpha,alpha-Diphenylpropionic acid beta-diethylaminoethyl ester2,2-diphenylpropionic acid 2-diethylaminoethyl esterАпрофен (Russian)
02

Targets

Nicotinic Acetylcholine ReceptormAChR (Muscarinic acetylcholine receptors)

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