GABA reuptake inhibitor

GABA reuptake inhibitor
Drug class
Tiagabine (Gabitril), a GABA transporter 1 (GAT-1) inhibitor and hence GABA reuptake inhibitor used as an anticonvulsant.
Class identifiers
SynonymsGRI; GABA uptake inhibitor; GABA transporter inhibitor; GABA transporter blocker; GAT inhibitor; GAT blocker
UseEpilepsy and other uses
Mechanism of actionGABA transporter inhibition
Biological targetGABA transporters
Chemical classGABA analogues and others
Legal status
In Wikidata

A GABA reuptake inhibitor (GRI), also known as a GABA transporter blocker, is a type of drug which acts as a reuptake inhibitor of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA) by blocking the action of one or more of the GABA transporters (GATs), such as the GABA transporter 1 (GAT-1). This in turn leads to increased extracellular concentrations of GABA and an increase in GABAergic neurotransmission.