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γ-Aminobutyric acid (GABA) neurotransmission is characterized by the restricted expression of the GABA-synthesizing enzyme glutamate decarboxylase (GAD), the GABA receptors, and the GABA transporters in GABAergic synapses consisting of a presynaptic nerve ending, a postsynaptic entity, and surrounding astrocytes (1). Additionally, the presynaptic nerve ending is characterized by the presence of the...
The system of GABA transporters in neural cells constitutes an efficient mechanism for terminating inhibitory GABAergic neurotransmission. As such these transporter are important therapeutical targets in epilepsy and potentially other neurological diseases related to the GABA system. In this study a number of analogs of 3-hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazol (exo-THPO), a promising...
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