Cookies

We use cookies to ensure that we give you the best experience on our website. You can change your cookie settings at any time. Otherwise, we'll assume you're OK to continue.


Durham Research Online
You are in:

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.

Abstract

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.
Publisher Web site:http://dx.doi.org/10.1016/S0028-3908(01)00191-5
Record Created:18 May 2007
Last Modified:19 Mar 2010 16:17

Social bookmarking: del.icio.usConnoteaBibSonomyCiteULikeFacebookTwitterExport: EndNote, Zotero | BibTex
Usage statisticsLook up in GoogleScholar | Find in a UK Library