4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.

@article{Pedregal20004AlkylA4,
  title={4-Alkyl- and 4-cinnamylglutamic acid analogues are potent GluR5 kainate receptor agonists.},
  author={Concepci{\'o}n Pedregal and Iluminada Corripio Collado and Alejandro Avello Escribano and Jes{\'u}s Ezquerra and Carmen Hern{\'a}ndez Dom{\'i}nguez and Ana I. Mateo and Almudena Rubio and Stephen R Baker and Jeffrey Goldsworthy and Rajender Kumar Kamboj and Barbara Ann Ballyk and K H Hoo and David Bleakman},
  journal={Journal of medicinal chemistry},
  year={2000},
  volume={43 10},
  pages={
          1958-68
        }
}
Enantiomerically pure (2S,4R)-4-substituted glutamic acids were prepared and tested for homomeric GluR5 and GluR6 kainate subtype receptor affinity. Some of the 4-cinnamyl analogues showed high selectivity and potency (K(i) < 25 nM) for the GluR5 receptors. The greatest selectivity and potency were achieved with the 3-(2-naphthyl)prop-2-enyl compound. This compound, LY339434, has negligible activity at the AMPA and kainate receptors GluR1, -2, -4 and -6. Although, LY339434 shows agonist… CONTINUE READING
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