Insights into structure-activity relationship of GABAA receptor modulating coumarins and furanocoumarins.

@article{Singhuber2011InsightsIS,
  title={Insights into structure-activity relationship of GABAA receptor modulating coumarins and furanocoumarins.},
  author={Judith Singhuber and Igor Baburin and Gerhard F. Ecker and Brigitte Kopp and Steffen Hering},
  journal={European journal of pharmacology},
  year={2011},
  volume={668 1-2},
  pages={
          57-64
        }
}
The coumarins imperatorin and osthole are known to exert anticonvulsant activity. We have therefore analyzed the modulation of GABA-induced chloride currents (I(GABA)) by a selection of 18 coumarin derivatives on recombinant α(1)β(2)γ(2S) GABA(A) receptors expressed in Xenopus laevis oocytes by means of the two-microelectrode voltage clamp technique. Osthole (EC(50)=14 ± 1 μM) and oxypeucedanin (EC(50)=25 ± 8 μM) displayed the highest efficiency with I(GABA) potentiation of 116 ± 4 % and 547… CONTINUE READING

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