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Discovery of non-zwitterionic GABA(A) receptor full agonists and a superagonist
Paul R Carlier1, Ella S-H Chow, Rebecca L Barlow
1Department of Chemistry, Virginia Tech, Blacksburg 24061, USA. pcarlier@vt.edu
Bioorganic & Medicinal Chemistry Letters
|July 13, 2002
Abstract:
Numerous previous studies of GABA(A) receptor ligands have suggested that GABA(A) receptor agonists must be zwitterionic and feature an intercharge separation similar to that of GABA (approx. 4.7-6A). In this communication we demonstrate that appropriately functionalized GABA amides are partial, full, or superagonists, despite their non-zwitterionic structure.