产品
编 号：F039631
分子式：C24H24N2O4
分子量：404.46
分子式：C24H24N2O4
分子量：404.46
产品类型
规格
价格
是否有货
结构图
CAS No: 111841-85-1
产品详情
生物活性：
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
体内研究：
Abecarnil (0.3 mg/kg, IP, once) antagonizes the brain neuroactive steroid increase induced by foot shock.Abecarnil (0-2.5 mg/kg, IP, once) dose dependently reduces epileptic activity.Abecarnil is effective against sound-induced convulsions in DBA/2 mice, against air blast-induced generalized seizures in gerbils and against myoclonus in baboons Papio papio.Abecarnil is 2-10 times more potent than DZP in most rodent tests of anxiolytic activity, and in reducing locomotor activity in mice and rats thoroughly habituated to the test chamber.Animal Model:Male Sprague-Dawley CD rats (200-250 g)
Dosage:0.3 mg/kg
Administration:IP, once, given 30 min before sacrifice
Result:Failed to change the basal pregnenolone and progesterone, while only slightly decreased THDOC levels, but antagonized the brain neuroactive steroid increase induced by foot shock.
Animal Model:WAG/Rij rats (male and female, 190-380 g, age 13-19 weeks, 8 rats each group)
Dosage:0, 0.16, 0.4, 1.0, and 2.5 mg/kg; 1 mL/400 g
Administration:IP, once
Result:Reduced the duration of spike-wave discharges and increased immobile behavior. Dose dependently reduced epileptic activity, whether measured as number, mean duration, or total duration of spike-wave discharges. The ED50 for reducing the number of spike-wave discharges in the second hour was 0.4 mg/kg.
体外研究：
Abecarnil enhances the binding of t-[35S]butylbicyclophosphorothionate to rat cortical membranes.Abecarnil exhibits a 3- to 6-fold higher affinity to forebrain BZ receptors than Diazepam (DZP).
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
体内研究：
Abecarnil (0.3 mg/kg, IP, once) antagonizes the brain neuroactive steroid increase induced by foot shock.Abecarnil (0-2.5 mg/kg, IP, once) dose dependently reduces epileptic activity.Abecarnil is effective against sound-induced convulsions in DBA/2 mice, against air blast-induced generalized seizures in gerbils and against myoclonus in baboons Papio papio.Abecarnil is 2-10 times more potent than DZP in most rodent tests of anxiolytic activity, and in reducing locomotor activity in mice and rats thoroughly habituated to the test chamber.Animal Model:Male Sprague-Dawley CD rats (200-250 g)
Dosage:0.3 mg/kg
Administration:IP, once, given 30 min before sacrifice
Result:Failed to change the basal pregnenolone and progesterone, while only slightly decreased THDOC levels, but antagonized the brain neuroactive steroid increase induced by foot shock.
Animal Model:WAG/Rij rats (male and female, 190-380 g, age 13-19 weeks, 8 rats each group)
Dosage:0, 0.16, 0.4, 1.0, and 2.5 mg/kg; 1 mL/400 g
Administration:IP, once
Result:Reduced the duration of spike-wave discharges and increased immobile behavior. Dose dependently reduced epileptic activity, whether measured as number, mean duration, or total duration of spike-wave discharges. The ED50 for reducing the number of spike-wave discharges in the second hour was 0.4 mg/kg.
体外研究：
Abecarnil enhances the binding of t-[35S]butylbicyclophosphorothionate to rat cortical membranes.Abecarnil exhibits a 3- to 6-fold higher affinity to forebrain BZ receptors than Diazepam (DZP).
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备