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Evaluation of Bicuculline as a GABA Antagonist

Abstract

THERE has been controversy recently about the reliability of bicuculline as an antagonist of the putative inhibitory transmitter γ-aminobutyric acid (GABA) in the brain1–3. Although the effects of bicuculline have so far been explained in terms of its combination with the GABA receptor, bicuculline might also affect the removal processes for GABA and the synthesis and release of endogenous GABA. We have therefore made quantitative analyses of the effects of iontophoretically applied bicuculline on the responses of neurones to GABA and have also estimated the effects of bicuculline on the concentration and turnover of GABA in the brain, GABA uptake and the synthetic and degradative enzymes glutamate decarboxylase (GAD) and 4-aminobutyrate : 2-oxoglutarate aminotransferase (GABA-T).

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STRAUGHAN, D., NEAL, M., SIMMONDS, M. et al. Evaluation of Bicuculline as a GABA Antagonist. Nature 233, 352–354 (1971). https://doi.org/10.1038/233352a0

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