Kynurenic acid analogues with improved affinity and selectivity for the glycine site on the N-methyl-D-aspartate receptor from rat brain.

@article{Foster1992KynurenicAA,
  title={Kynurenic acid analogues with improved affinity and selectivity for the glycine site on the N-methyl-D-aspartate receptor from rat brain.},
  author={Alan C. Foster and John A. Kemp and Paul D. Leeson and Sarah Grimwood and Ann E Donald and Garland R. Marshall and Tony Priestley and John D. Smith and Robert W Carling},
  journal={Molecular pharmacology},
  year={1992},
  volume={41 5},
  pages={914-22}
}
The glycine site on the N-methyl-D-aspartate (NMDA) subtype of receptors for the excitatory neurotransmitter glutamate is a potential target for the development of neuroprotective drugs. We report here two chemical series of glycine site antagonists derived from kynurenic acid (KYNA), with greatly improved potency and selectivity. Disubstitution with chlorine or bromine in the 5- and 7-positions of KYNA increased affinity for [3H]glycine binding sites in rat cortex/hippocampus P2 membranes… CONTINUE READING

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