Paula Zaręba, Beata Gryzło, Gabriela Mazur and Barbara Malawska* Pages 750 - 776 ( 27 )
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.
GABA transporters, GAT1, BGT1, GAT2, GAT3, GABA uptake inhibitors.
Department of Physicochemical Drug Analysis, Chair of Pharmaceutical Chemistry, Jagiellonian University Medical College, 9 Medyczna St, 30-688 Krakow, Department of Organic Chemistry, Faculty of Pharmacy, Jagiellonian University Medical College, 9 Medyczna St, 30-688 Krakow, Department of Physicochemical Drug Analysis, Chair of Pharmaceutical Chemistry, Jagiellonian University Medical College, 9 Medyczna St, 30-688 Krakow, Department of Physicochemical Drug Analysis, Chair of Pharmaceutical Chemistry, Jagiellonian University Medical College, 9 Medyczna St, 30-688 Krakow