Abecarnil (ZK 112119) 是一种benzodiazepine (BZ)受体的配体或部分激动剂。Abecarnil 具有抗惊厥和抗焦虑的特性。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 具有抗癫痫的研究潜力。

Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor, possessing anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABA A receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC 50 of 0.82 nM. Abecarnil can be used for epilepsy research [1] [2] [3] [4].

Abecarnil enhances the binding of t-[35S]butylbicyclophosphorothionate to rat cortical membranes [1]. In vivo, Abecarnil shows a 3- to 6-fold higher affinity to forebrain BZ receptors than Diazepam (DZP) [1].

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 lowers 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]. In most rodent tests of anxiolytic activity, Abecarnil is 2-10 times more potent than DZP, 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 ED 50 for reducing the number of spike-wave discharges in the second hour was 0.4 mg/kg.

111841-85-1

C24H24N2O4

404.46

Abecarnil

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years