CI-966

Research use only, not for human use.

CI-966 (PD 126141) is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively.

CI-966 (PD 126141) is a potent, selective inhibitor of the GABA transporter GAT-1 with IC50 of 0.26 and 1.2 uM for human and rat GAT-1, respectively; displays >200-fold selectivity over GAT-2 and GAT-3; shows anticonvulsive and neuroprotective activity in vivo.Epilepsy Phase 1 Discontinued.

CI-966 functions by selectively inhibiting GABA reuptake in neurons and glial cells.

CI-966 produces intermediate levels of Pentylenetetrazol (PTZ)-lever responding when administered to PTZ-trained rats.CI-966 enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. CI-966 is administered systemically by i.p. injection (5 mg/kg) in Sprague-Dawley rats under urethane anaesthesia. Twenty to thirty minutes after injection there is a highly variable, but overall significant, enhancement of the inhibition of hippocampal population spikes by GABA applied by microiontophoresis in the CA1 region. CI-966 exhibits anticonvulsant properties in various animal models. Oral absorption of CI-966 in dogs given 1.39 mg/kg is rapid with a tmax of 0.7 hr.In rats given 5 mg/kg oral, a mean tmax of 4.0 hr is observed. Following i.v. administration of the same respective doses, elimination t1/2 in dogs and rats averages 1.2 and 4.5 hr. Absolute oral bioavailability of CI-966 is 100% in both species. Animal Model:Eight male Sprague-Dawley rats Dosage:0.3-30 mg/kg Administration:Injection IP in a volume of 1 mL/kg Result:Dose dependent decreases in rates of responding occurred following CI-966 administration.

PD 126141

Membrane Transporter/Ion Channel

GAT

GAT

Neurological Disease

Epilepsy

110283-79-9

473.415

C23H21F6NO3

>98% (HPLC)

——

C1CN(CC(=C1)C(=O)O)CCOC(C2=CC=C(C=C2)C(F)(F)F)C3=CC=C(C=C3)C(F)(F)F

1-[2-[bis[4-(Trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years