Historical note and terminology
Tiagabine, as a novel antiepileptic, has a mechanism of action related to GABA. The synthesis of vigabatrin (gamma-vinyl-GABA) was a result of a rational approach to design compounds to inhibit the major GABA-degrading enzyme, GABA transaminase. Whereas vigabatrin is a selective and irreversible GABA-transaminase inhibitor that greatly increases whole-brain levels of GABA, tiagabine is a potent inhibitor of GABA uptake into neurons and glial cells.
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