Inhibition of γ-aminobutyric acid uptake by bicuculline analogues

Julianna Kardos, Ilona Kovács, Tamás Blandl, Derek J. Cash, Edit Simon-Trompler, Nguyen D. Luyen, Gábor Dörnyei, Miklós Simonyi, Gábor Blaskó, Csaba Szántay

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Enantiomers of norbicuculline, (+)[1S,9R] and (-)[1R,9S]erythro-1-[1'-(4',5'-methylenedioxyphthalidyl)]-6,7-methylendedioxy -1,2,3,4-tetrahydroisoquinoline and of the N-methyl derivatives {(+)[1S,9R] and (-)[1R,9S)]bicuculline} were found to inhibit the progress of the γ-aminobutyric acid transporter-mediated uptake of 40 μM [14C]γ-aminobutyric acid into native plasma membrane vesicles from the rat cerebral cortex at 30°C. The values for the dissociation constants of the reversible inhibition, relative to (+)[1S,9R]bicuculline, in order of increasing inhibition, were: (-)[1R,9S]bicuculline, 3.3; (+)[1S,9R]-bicuculline, 1.0; (-)[1R,9S]norbicuculline, 0.4 ~ (+)[1S,9R]norbicuculline; guvacine, 0.02. The norbicucullines have higher potencies than (+)[1S,9R]bicuculline for the γ-aminobutyric acid transporter, in contrast to the relative potencies of these inhibitors for the inhibition of function and γ-aminobutyric acid binding of the γ-aminobutyric acid type A receptor.

Original languageEnglish
Pages (from-to)83-86
Number of pages4
JournalEuropean Journal of Pharmacology
Issue number1
Publication statusPublished - Oct 15 1997


  • Bicuculline analogue, enantiomer
  • Cortex
  • Rat
  • Uptake, quench flow
  • [C]GABA ([C]γ-aminobutyric acid)

ASJC Scopus subject areas

  • Pharmacology

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    Kardos, J., Kovács, I., Blandl, T., Cash, D. J., Simon-Trompler, E., Luyen, N. D., Dörnyei, G., Simonyi, M., Blaskó, G., & Szántay, C. (1997). Inhibition of γ-aminobutyric acid uptake by bicuculline analogues. European Journal of Pharmacology, 337(1), 83-86.