A potent GABA uptake inhibitor, selective for GAT-1 (IC50
values are 0.13, 550, 944 and 7210 μ
M for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). Inhibits transport current competitively (Ki
= 7 μ
M) and transmitter-gated current non-competitively (Ki
= 0.03 nM). Able to pass the blood-brain barrier after systemic administration and is active in vivo
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Sold with the permission of GlaxoSmithKline
Orally active and potent inhibitors of γ-aminobutyric acid.
Ali et al.
Identification and selective inhibition of the channel mode of the neuronal GABA transporter 1.
Krause and Schwarz
On the bioactive conformation of the GABA uptake inhibitor SK&F 89976-A.