Discovery of non-Zwitterionic GABAA receptor full agonists and a superagonist

Numerous previous studies of GABAA receptor ligands have suggested that GABAA receptor agonists must be zwitterionic and feature an intercharge separation similar to that of GABA (approx. 4.7–6 Å). In this communication we demonstrate that appropriately functionalized GABA amides are partial, full, or superagonists, despite their non-zwitterionic structure.