New Highly Potent GABA Uptake Inhibitors Selective for GAT-1 and GAT-3 Derived from (R)-and (S)-Proline and Homologous Pyrrolidine-2-alkanoic Acids.-Enantiomerically pure N-substituted proline and pyrolidinealkanoic acid derivatives are synthesized and evaluated for their affinity at the GABA transport proteins GAT-1 and GAT-3 with a special emphasis on enantioselectivity of binding and subtype specificity. Among the N-substituted derivatives, pyrrolidines (VII) exhibit the highest affinity to the GAT-1 protein, whereas pyrrolidine (IX) displays excellent inhibitory activity at GAT-3 with a high subtype selectivity with regard to GAT-1. -(FUELEP, G. H.; HOESL, C. E.; HOEFNER, G.; WANNER*, K. T.; Eur.
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