Abecarnil (ZK 112119) 是一种benzodiazepine (BZ)受体的配体或部分激动剂。Abecarnil 具有抗焦虑和抗惊厥的特性。Abecarnil 可作为GABAA受体的正变构调节剂。Abecarnil 可抑制 BZ [3H]lormetazepam 与大鼠大脑皮层膜的结合，其IC50为 0.82 nM。Abecarnil 可用于癫痫的研究。
| 生物活性 | Abecarnil (ZK 112119) is a ligand or a partial agonist forbenzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator ofGABAAreceptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with anIC50of 0.82 nM. Abecarnil can be used for epilepsy research[1][2][3][4]. |
体外研究
(In Vitro) | Abecarnil enhances the binding of t-[35S]butylbicyclophosphorothionate to rat cortical membranes[1].
Abecarnil exhibits a 3- to 6-fold higher affinity to forebrain BZ receptors than Diazepam (DZP)[1].
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体内研究
(In Vivo) | Abecarnil (0.3 mg/kg, IP, once) antagonizes the brain neuroactive steroid increase induced by foot shock[2].
Abecarnil (0-2.5 mg/kg, IP, once) dose dependently reduces epileptic activity[3].
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[4].
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[1].
| Animal Model: | Male Sprague-Dawley CD rats (200-250 g)[2] | | 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)[3] | | 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 ED50for reducing the number of spike-wave discharges in the second hour was 0.4 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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