Alcohol
Volume 20, Issue 3 , Pages 227-236, April 2000

Design and structure-activity relationship analysis of ligands of gamma-hydroxybutyric acid receptors

Laboratoire de Pharmacochimie de la Communication Cellulaire, ERS 655 du CNRS, Faculté de Pharmacie, 74 route du Rhin, B.P. 21, Illkirch, 67401, France

Received 25 May 1998; received in revised form 6 July 1998; accepted 13 July 1998.

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).

Keywords:  Gamma-hydroxybutyric acid, Derivatives, Lactone, Alcohol, Drug design, Crotonic acids, Ligands, Receptors, Antagonist

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PII: S0741-8329(99)00086-5

Alcohol
Volume 20, Issue 3 , Pages 227-236, April 2000

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