Discovery of non-zwitterionic GABA(A) receptor full agonists and a superagonist |
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| Authors: | Carlier Paul R Chow Ella S-H Barlow Rebecca L Bloomquist Jeffrey R |
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| Affiliation: | Department of Chemistry, Virginia Tech, Blacksburg 24061, USA. pcarlier@vt.edu |
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| 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. |
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