Tiagabine hydrochloride | GABA transporter 1 (GAT1) inhibitor

Tiagabine (145821-59-6) is a clinically useful anticonvulsant.¹ It is also used to treat anxiety/panic disorder² and neuropathic pain³. Tiagabine inhibits GABA-reuptake (IC₅₀ [³H]GABA uptake = 67 nM) via inhibiting GABA transporter 1(GAT1) blocking both neuronal and glial GABA re-uptake.^4,5

References/Citations
1) Schacter (1999) A Review of the Antiepileptic Drug Tiagabine, Clin. Neuropharmacol. 22 312
2) Schwartz and Nihalani (2006) Tiagabine in anxiety disorders, Expert Opin. Pharmacother. 7 1977
3) Novak et al. (2001) Treatment of Painful Sensory Neuropathy With Tiagabine: A Pilot Study, Clin. Auton. Res. 11 357
4) Braestrup et al. (1990) (R)-N-[4,4-bis(3-methyl-2-thienyl)but-3-en-1-yl)nipecotic Acid Binds With High Affinity to the Brain Gamma-Aminobutyric Acid Uptake Carrier, J. Neurochem. 54 639
5) Nielsen et al. (1991) Characterization of Tiagabine (NO-328), a New Potent and Selective GABA Uptake Inhibitor, Eur. J. Pharmacol. 196 257