top of page
The Sound of Evolution
Tiagabine
Mechanism of action:
Tiagabine is a selective GABA reuptake inhibitor. Tiagabine selectively inhibits GABA transporter-1 (GAT-1) on neurons and glial cell membranes, preventing GABA from being reabsorbed from the synaptic cleft into cells. This increases the concentration of GABA in the synaptic cleft and prolongs its duration of action, thereby enhancing inhibitory signaling through both GABA_A and GABA_B receptors.
Reference(s):
1. Chen X et al. (2002). TTD: Therapeutic Target Database. Nucleic Acids Res.
2. Pollack MH et al. (2005). The selective GABA reuptake inhibitor tiagabine for the treatment of generalized anxiety disorder: results of a placebo-controlled study. J Clin Psychiatry.
bottom of page