Imepitoin

Description: Imepitoin, formerly known as AWD 131-138 and ELB 138, is a novel partial BZD (benzodiazepine) receptor agonist that has the potential use as an antiepileptic drug for the treatment of canine idiopathic epilepsy. Imepitoin is a centrally acting anti-epileptic which crosses the blood brain barrier. It inhibits seizures via potentiation of the GABA a receptor-mediated inhibitory effects on the neurones. Imepitoin exerts significant anticonvulsant efficacy without tolerance in a dog seizure model as well as in epileptic dogs with spontaneously recurrent seizures. These data thus substantiate that partial agonism at the BZD site of GABAA receptors offers advantages versus full agonism and constitutes a valuable approach for treatment of seizures.

References: Epilepsia. 2004 Oct; 45(10):1228-39.