CI-966 hydrochloride

Research use only, not for human use.

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

CI-966 hydrochloride produces intermediate levels of Pentylenetetrazol (PTZ)-lever responding when administered to PTZ-trained rats.CI-966 hydrochloride enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. CI-966 hydrochloride 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 hydrochloride exhibits anticonvulsant properties in various animal models. Oral absorption of CI-966 hydrochloride 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 hydrochloride is 100% in both species. Animal Model:Eight male Sprague-Dawley ratsDosage: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.

CI966

Membrane Transporter/Ion Channel

GAT

GAT

——

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110283-66-4

509.873

C23H22ClF6NO3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (98.06 mM)

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.Cl

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

(-20℃)

With Ice Pack

≥ 2 years