产品
编 号：F036394
分子式：C23H22ClF6NO3
分子量：509.87
分子式：C23H22ClF6NO3
分子量：509.87
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 110283-66-4
产品详情
生物活性：
CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.
体内研究：
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 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.
体外研究：
CI-966 hydrochloride functions by selectively inhibiting GABA reuptake in neurons and glial cells.
CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.
体内研究：
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 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.
体外研究：
CI-966 hydrochloride functions by selectively inhibiting GABA reuptake in neurons and glial cells.
产品资料
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