The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitro.

@article{Olpe1993TheAO,
  title={The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitro.},
  author={Hans Rudolf Olpe and Martin W. Steinmann and T. Ferrat and Mario F. Pozza and Karin Greiner and Felix Brugger and Wolfgang Froestl and Stuart J. Mickel and Helmut Bittiger},
  journal={European journal of pharmacology},
  year={1993},
  volume={233 2-3},
  pages={179-86}
}
The goal of this report is to present the results obtained with three new GABAB receptor antagonists. CGP 54062 has an IC50 in a GABAB binding test of 0.013 microM which is roughly 2500-fold lower than one of the most potent blockers known so far, CGP 35348 (IC50 = 34 microM). CGP 46381 and CGP 36742 have IC50s of 4.9 and 36 microM respectively. The latter two compounds are the first orally active GABAB receptor antagonists. All three compounds bind to the GABAB receptor selectively, and are… CONTINUE READING
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