A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.

@article{Selvam2010AVS,
  title={A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.},
  author={Chelliah Selvam and Nadia Oueslati and Isabelle Anne Lemasson and Isabelle Brabet and Delphine Rigault and Tiphanie Courtiol and Sara Cesarini and Nicolas Triballeau and Hugues-Olivier Bertrand and Cyril Goudet and Jean-Philippe Pin and Francine C Acher},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 7},
  pages={
          2797-813
        }
}
(R)-PCEP (3-amino-3-carboxypropyl-2'-carboxyethyl phosphinic acid, 1), a new metabotropic glutamate receptor 4 (mGlu4R) agonist, was discovered in a previously reported virtual screening. The (S)-enantiomer and a series of derivatives were synthesized and tested on recombinant mGlu4 receptors. A large number of derivatives activated this receptor but was not able to discriminate between mGlu4 and mGlu8 receptors. The most potent ones 6 and 12 displayed an EC(50) of 1.0 +/- 0.2 microM at mGlu4R… CONTINUE READING
BETA

Citations

Publications citing this paper.
SHOWING 1-10 OF 25 CITATIONS

References

Publications referenced by this paper.
SHOWING 1-10 OF 52 REFERENCES

Positive and negativemodulation of group Imetabotropic glutamate receptors

  • S. uller, M. Hechenberger, +10 authors T. Weil
  • J. Med. Chem
  • 2008

Similar Papers

Loading similar papers…