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. 1991 Jun;103(2):1385–1392. doi: 10.1111/j.1476-5381.1991.tb09799.x

The pharmacological specificity of N-methyl-D-aspartate receptors in rat cerebral cortex: correspondence between radioligand binding and electrophysiological measurements.

S Grimwood 1, A C Foster 1, J A Kemp 1
PMCID: PMC1908363  PMID: 1832067

Abstract

1. The pharmacological specificity of N-methyl-D-aspartate (NMDA) receptors has been investigated in the rat cerebral cortex by use of radioligand binding and electrophysiological techniques. 2. A comparison was made between a functional assay (NMDA-induced depolarizations in a rat cortical slice preparation) and NMDA-sensitive L-[3H]-glutamate binding in the same brain region and species, to provide accurate affinity values for agonists and antagonists at the NMDA recognition site. 3. In a preparation of crude postsynaptic densities (PSD) from rat cortex, L-[3H]-glutamate bound with high affinity to an NMDA-sensitive population of sites with KD (geometric mean (-s.e.mean. + s.e. mean) = 120 (114, 126) nM, Bmax (mean +/- s.e.mean) = 11.4 +/- 0.8 pmol mg-1 protein and Hill coefficient (mean +/- s.e.mean) = 1.2 +/- 0.17 (n = 3). 4. There was a good agreement between the relative affinities in radioligand binding and electrophysiological assays for the receptor agonists NMDA, N-methyl-L-aspartate, quinolinate and trans-2,3-piperidine dicarboxylate, which are poor substrates of acidic amino acid transport systems. However, agonists which are good substrates for high affinity uptake systems (L- and D-glutamate, L- and D-aspartate, D-aspartate-beta-hydroxamate and L-glutamate-gamma-hydroxamate) were much weaker in the electrophysiological experiments.(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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