The fine-tuning and homeostatic balance of the GABAergic inhibitory tone in the central
nervous system (CNS) is a prerequisite for controlling the excitatory neurotransmission. This …

The identification and subsequent development of the GABA transport inhibitor tiagabine has
confirmed the important role that GABA transporters play in the control of CNS excitability. …

A series of lipophilic diaromatic derivatives of the glia-selective GABA uptake inhibitor (R)-4-amino-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol
[(R)-exo-THPO, 4] were synthesized via …

In a recent study, EF1502 [N-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-hydroxy-4-(methylamino)-4,5,6,7-tetrahydrobenzo
[d]isoxazol-3-ol], which is an N-substituted analog of the GAT1-…

The inhibitory effect of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole (exo-THPO)
and its N-methylated (N-methyl-exo-THPO) andN-ethylated (N-ethyl-exo-THPO) analogs, …

The adaptation of cells to hyperosmotic conditions involves accumulation of organic
osmolytes to achieve osmotic equilibrium and maintenance of cell volume. The Na + and Cl − -…

Inactivation of γ-aminobutric acid (GABA) as a neurotransmitter is mediated by diffusion in the
synaptic cleft followed by binding to transporter sites and translocation into the intracellular …

The system of GABA transporters in neural cells constitutes an efficient mechanism for
terminating inhibitory GABAergic neurotransmission. As such these transporter are important …

γ-Aminobutyric acid (GABA) neurotransmission is characterized by the restricted expression
of the GABA-synthesizing enzyme glutamate decarboxylase (GAD), the GABA receptors, …

A powerful collection of readily reproducible cutting-edge techniques for characterizing the
ligand or substrate binding of neurotransmitter receptors and transporters. The procedures …