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Studies on the subtype selectivity of CP-101,606 : evidence for two classes of NR2B-selective NMDA receptor antagonists.

Chazot, P. L. and Lawrence, S. and Thompson, C. L. (2002) 'Studies on the subtype selectivity of CP-101,606 : evidence for two classes of NR2B-selective NMDA receptor antagonists.', Neuropharmacology., 42 (3). pp. 319-324.


The subtype-selectivity of racemic [3H]CP-101,606, a novel high-affinity NMDA receptor radioligand was determined using defined recombinant NMDA receptor subunits expressed in HEK 293 cells. [3H]CP-101,606 binds to adult rodent forebrain and NR1/NR2B receptors expressed in HEK 293 cells with KD=4.2 nM and 6.0 nM, respectively. In contrast, no high affinity specific binding was detected to NR1, NR2A, NR2B subunits expressed alone or NR1/NR2A receptors. HEK 293 cells were transfected with NR1, NR2A and NR2B receptor subunits and complexes comprising all three subunits were isolated by anti-NR2A immunoaffinity chromatography. Based on immunoblotting with subunit-selective antibodies, the immunopurified material contained all three NMDA receptor subunit polypeptides. However, in contrast to parallel studies in which high affinity [3H]Ro-25,6981 binding activity was observed, no high affinity [3H]CP-101,606 binding sites were detected to the immunopurified material. This study provides further evidence for two distinct classes of NR2B-directed NMDA receptor antagonists, one which binds with high affinity irrespective whether another NR2 subunit type is present (Ro-25,6981) and a second class which is affected significantly by the presence of another NR2 subunit type within the receptor complex, exemplified by CP-101,606.

Item Type:Article
Keywords:NR1/NR2A/NR2B, NMDA receptor, Racemic [3H]CP-101,606, Immunoaffinity chromatography, Subtype-selectivity.
Full text:Full text not available from this repository.
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Date accepted:No date available
Date deposited:No date available
Date of first online publication:March 2002
Date first made open access:No date available

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