Selective inhibitor of the GABA transporter GAT-1 (IC50
values are 0.26 and 1.2 μ
M at cloned human and rat GAT-1 respectively). Displays over 200-fold selectivity over GAT-2 and GAT-3. Centrally active upon systemic administration in vivo
. Anticonvulsive and neuroprotective.
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.
Systemic CI-966, a new gamma-aminobutyric acid uptake blocker, enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ.
Ebert et al.
Pharmacokinetics, mass balance, and induction potential of novel GABA uptake inhibitor, CI-966 HCl, in laboratory animals.
Radulovic et al.
Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.
Borden et al.