CI 966 hydrochloride
Chemical Name: 1-[2-[bis[4-(Trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride
Purity: ≥98%
Biological Activity
CI 966 hydrochloride is a selective inhibitor of the GABA transporter GAT-1 (IC50 values are 0.26 and 1.2 μM 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Systemic CI-966, a new gamma-aminobutyric acid uptake blocker, enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ.
Ebert et al.
Can.J.Physiol.Pharmacol., 1990;68:1194 -
Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1.
Borden et al.
Eur.J.Pharmacol., 1994;269:219 -
Pharmacokinetics, mass balance, and induction potential of novel GABA uptake inhibitor, CI-966 HCl, in laboratory animals.
Radulovic et al.
Pharm.Res., 1993;10:1442
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