Neurotransmitter Transporters and Anticonvulsant Drug Development
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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.
