Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.

@article{Bueno2005DipeptidesAE,
  title={Dipeptides as effective prodrugs of the unnatural amino acid (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740), a selective group II metabotropic glutamate receptor agonist.},
  author={Ana B Bueno and Iv{\'a}n Collado and Alfonso de Dios and C. S. H. Dom{\'i}nguez and Jos{\'e} Alfredo Mart{\'i}n and Luisa M Mart{\'i}n and Mar{\'i}a Angeles Mart{\'i}nez-Grau and Carlos Montero and Concepci{\'o}n Pedregal and John Catlow and D Scott Coffey and Michael P Clay and Anne H. Dantzig and Terry Lindstrom and James A. Monn and HaiYan Jiang and Darryle D. Schoepp and Robert E. Stratford and Linda B. Tabas and Joseph P. Tizzano and Rebecca A. Wright and Marc F. Herin},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 16},
  pages={5305-20}
}
(+)-2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (1), also known as LY354740, is a highly potent and selective agonist for group II metabotropic glutamate receptors (mGlu receptors 2 and 3) tested in clinical trials. It has been shown to block anxiety in the fear-potentiated startle model. Its relatively low bioavailability in different animal species drove the need for an effective prodrug form that would produce a therapeutic response at lower doses for the treatment of anxiety disorders… CONTINUE READING

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