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Design and structure-activity relationship analysis of ligands of gamma-hydroxybutyric acid receptors
J J Bourguignon1, M Schmitt, B Didier
1Laboratoire de Pharmacochimie de la Communication Cellulaire, ERS 655 du CNRS, Faculté de Pharmacie, 74 route du Rhin, B.P. 21, 67401, Illkirch, France. jjb@pharma.u-strasbg.fr
Abstract:
With the use of [3H]gamma-hydroxybutyric acid, binding experiments allowed the screening of new compounds as ligands of gamma-hydroxybutyric acid receptors. Starting from the acid-alcohol gamma-hydroxybutyric acid structure, structure-activity relation analysis and lead optimization highlighted gamma-hydroxybutyric acid derivatives with significantly increased affinities, when compared with the affinity of gamma-hydroxybutyric acid. Further pharmacological studies with the use of gamma-hydroxybutyric acid derivatives allowed the characterization of the first competitive antagonist acting at gamma-hydroxybutyric acid receptors (NCS 382).