CI-966 hydrochloride produces intermediate levels of Pentylenetetrazol (PTZ)-lever responding when administered to PTZ-trained rats[4].
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[5].
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[6].
| Animal Model: | Eight male Sprague-Dawley rats[4] |
| 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.
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