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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemistry*
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Amides / metabolism
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Amides / pharmacology*
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Animals
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Binding, Competitive
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Chlorides / metabolism
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Dimerization
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Dose-Response Relationship, Drug
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GABA-A Receptor Agonists*
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Ligands
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Mice
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Protein Binding
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Receptors, GABA-A / metabolism
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Structure-Activity Relationship
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Synaptosomes / drug effects
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Synaptosomes / physiology
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gamma-Aminobutyric Acid / analogs & derivatives*
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gamma-Aminobutyric Acid / metabolism
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gamma-Aminobutyric Acid / pharmacology
Substances
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Amides
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Chlorides
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GABA-A Receptor Agonists
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Ligands
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Receptors, GABA-A
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gamma-Aminobutyric Acid