Abecarnil

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 GABA_A 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^[1][2][3][4]. 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]. 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].