Neurotransmitter transporters and anticonvulsant drug development

Abstract

Excitatory and inhibitory neurotransmission mediated by glutamate and GABA, respectively, plays a major role in generation of seizures. So far, emphasis has been placed on the GABA system in attempts to develop antiepileptic drugs. Tiagabine, a selective inhibitor of GABA transporter 1 (GAT1), is marketed for treatment of certain seizure types and serves as a proof of principle that inhibitors of GABA transport may be interesting in this context. The chapter describes the methodology available to investigate in detail the pharmacology of GABA transporters and design of studies leading to identification of drug candidates. Emphasis is placed on a possible role of extrasynaptic GABA transporters in seizure control. © 2011 Springer Science+Business Media, LLC.