1. Development, Recent Achievements and Current Directions of Research into GABA Uptake Inhibitors
- Author
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Barbara Malawska, Paula Zaręba, Gabriela Mazur, and Beata Gryzło
- Subjects
GABA Plasma Membrane Transport Proteins ,Central nervous system ,Subtype selectivity ,Neurotransmission ,Synaptic Transmission ,01 natural sciences ,Biochemistry ,Cell membrane ,03 medical and health sciences ,chemistry.chemical_compound ,Drug Discovery ,medicine ,Animals ,0101 mathematics ,Neurotransmitter ,gamma-Aminobutyric Acid ,030304 developmental biology ,Pharmacology ,0303 health sciences ,Physiological function ,Chemistry ,Organic Chemistry ,Biological Transport ,Transporter ,010101 applied mathematics ,medicine.anatomical_structure ,Molecular Medicine ,GABA Uptake Inhibitors ,Neuroscience - Abstract
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.
- Published
- 2021
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