| 8223944 |
Johansen TH, Drejer J, Watjen F, Nielsen EO: A novel non-NMDA receptor antagonist shows selective displacement of low-affinity [3H] kainate binding. Eur J Pharmacol. 1993 Aug 15;246(3):195-204.
5-Nitro-6,7,8,9-tetrahydrobenzo [G] indole-2,3-dione-3-oxime (NS-102), a new competitive glutamate receptor antagonist displaced binding to non-N-methyl-D-aspartate (non-NMDA) binding sites with no activity at the NMDA and strychnine-insensitive glycine binding sites. Under experimental conditions in which both high- and low-affinity sites were labelled, NS-102 only partially inhibited the binding of [3H] kainate. Studies of NS-102 displacement of high-affinity versus low-affinity [3H] kainate binding showed a high selectivity of NS-102 for the low-affinity [3H] kainate binding site (Ki = 0.6 microM) compared to the high-affinity [3H] kainate binding site (Ki > 10 microM). NS-102 was a relatively weak inhibitor of 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl) propionic acid (AMPA) binding (IC50 = 7.2 microM). NS-102 and related compounds with similar pharmacological profiles may become valuable tools in the characterization of the functional importance of the low-affinity [3H] kainate binding site. |
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