Drug intelligence / Profile preview

aprobarbital

Development stage
Discontinued
Modality
Small Molecules
Administration
Oral
01

Overview

Aprobarbital is a barbiturate derivative synthesized in the 1920s by Ernst Preiswerk. It possesses sedative, hypnotic, and anticonvulsant properties and was primarily used for the treatment of insomnia. Aprobarbital acts as a central nervous system depressant by binding to the Gamma-aminobutyric acid type A receptor (GABAA receptor) at either the alpha or beta subunit—distinct from both GABA itself and benzodiazepine binding sites—thereby potentiating GABAergic inhibition. This results in increased amplitude and decay time of inhibitory postsynaptic currents. Additionally, aprobarbital blocks AMPA receptors (a subtype of glutamate receptor) and appears to bind neuronal nicotinic acetylcholine receptors. Its use has largely been replaced by safer alternatives such as benzodiazepines[1][2][3][4][5].

Brand names
OramonSomnifaineAllonal
Other names
aprobarbitoneallylpropymalAlurate5-isopropyl-5-allylbarbituric acid
02

Targets

AMPAR (AMPA receptor)Nicotinic Acetylcholine ReceptorGABAA (Gamma-aminobutyric acid receptor)

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