| Bioactivity | 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[1][2][3][4]. |
| Invitro | 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]. Animal Model: |
| Name | Abecarnil |
| CAS | 111841-85-1 |
| Formula | C24H24N2O4 |
| Molar Mass | 404.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Stephens DN, et al. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors. J Pharmacol Exp Ther. 1990 Apr;253(1):334-43. [2]. Barbaccia ML, et al. Stress-induced increase in brain neuroactive steroids: antagonism by abecarnil. Pharmacol Biochem Behav. 1996 May;54(1):205-10. [3]. Coenen AM, et al. Effects of the beta-carboline abecarnil on epileptic activity, EEG, sleep and behavior of rats. Pharmacol Biochem Behav. 1992 Jul;42(3):401-5. [4]. Turski L, et al. Anticonvulsant action of the beta-carboline abecarnil: studies in rodents and baboon, Papio papio. J Pharmacol Exp Ther. 1990 Apr;253(1):344-52. |