Neurotransmitter γ-aminobutyric acid (GABA) plays a principal role in the regulation of
mammalian central nervous system functions. GABA evoked neurotransmission is terminated by a
rapid uptake via dependent plasma membrane GABA transporters (GATs) located in the cell
membrane. Potent inhibitors of these GATs are of fundamental importance for elucidation of the
physiological function of these targets. Over recent years, a wide range of new GAT1-selective and
less common non-GAT1-selective inhibitors have been successfully developed. This review
highlights development and recent significant achievements in the field of GABA reuptake inhibitors.
Special attention is paid to their pharmacological roles, structure and subtype selectivity relationships.
Keywords: GABA transporters, GAT1, BGT1, GAT2, GAT3, GABA uptake inhibitors.
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