European Journal of Pharmacology 1997-02-19

In vivo modulation of benzodiazepine receptor function after inhibition of endogenous gamma-aminobutyyric acid synthesis.

M Bottlaender, L Schmid, C Fuseau, D Fournier, E Brouillet, M Mazière

Index: Eur. J. Pharmacol. 321 , 13, (1997)

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Abstract

The influence of decreased endogenous gamma-aminobutyric acid (GABA) concentration on benzodiazepine receptor function was studied in the brain of living baboons. Positron emission tomography and the radiotracer [11C]flumazenil combined with electroencephalography were used to determine the pharmacological properties of two bezodiazepine receptors agonists, diazepam and bretazenil, in baboons pre-treated or not with DL-allylglycine (an inhibitor of GABA synthesis). Our results show that, in vivo, DL-allylglycine reduces the affinity of benzodiazepine receptors for their agonists without altering the intrinsic capability of agonists to allosterically modulate GABAergic transmission.