New GABA amides activating GABA_A-receptors

• Peter Raster,
• Andreas Späth,
• Svetlana Bultakova,
• Pau Gorostiza,
• Burkhard König and
• Piotr Bregestovski

Beilstein J. Org. Chem. 2013, 9, 406–410, doi:10.3762/bjoc.9.42

• of Catalonia (IBEC) and Institució Catalana de Recerca i Estudis Avançats (ICREA), 08028 Barcelona, Spain 10.3762/bjoc.9.42 Abstract We have prepared a series of new and some literature-reported GABA-amides and determined their effect on the activation of GABAA-receptors expressed in CHO cells

• . Special attention was paid to the purification of the target compounds to remove even traces of GABA contaminations, which may arise from deprotection steps in the synthesis. GABA-amides were previously reported to be partial, full or superagonists. In our hands these compounds were not able to activate

• GABAA-receptor channels in whole-cell patch-clamp recordings. New GABA-amides, however, gave moderate activation responses with a clear structure–activity relationship suggesting some of these compounds as promising molecular tools for the functional analysis of GABAA-receptors. Keywords: CHO-cells