Tiagabine hydrochloride is an anticonvulsant agent and a selective inhibitor of the GAT-1 GABA transporter, with a Ki of approximately 0.1 μM. It potently and selectively inhibits GABA reuptake with IC50s of 67, 446, and 182 nM for [3H]GABA uptake in synaptosomes, neurons, and glia. This compound also exhibits neuroprotective properties.
- Selective inhibitor of GAT-1 GABA transporter
- Potently and selectively inhibits GABA reuptake
- Exhibits neuroprotective properties
- Protects neurons against mutant huntingtin-induced toxicity
- Increases viability of SH-SY5Y cells
- Neuroprotective in mouse models of Huntington's disease
- Reduces dopaminergic neuronal loss in PD mouse models
- Shows anti-allodynic effect in a rat model of neuropathic pain
- Antinociceptive effects against acute thermal pain in mice
- Suppresses pentylenetetrazole-induced seizures and improves cognitive parameters in mice