Journal
NEUROSCIENCE LETTERS
Volume 451, Issue 1, Pages 29-33Publisher
ELSEVIER IRELAND LTD
DOI: 10.1016/j.neulet.2008.12.036
Keywords
NMDA receptors; Ion channel blockade; Structure-function relationships
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Funding
- RFBR [0804-00326, 070400617]
- Russian Scientific School [4821.2008.4]
- RAS program Molecular and Cell Biology
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9-Aminoacridine is known as foot-in-the-door NMDA receptor channel blocker because its binding prevents channel closure. Structural determinants of this mechanism of block were studied using a series of 9-aminoacridine derivatives. Experiments were performed on native NMDA receptors of hippocampal pyramidal neurons, isolated from rat brain slices. The use-dependence of block and kinetics of recovery from block were used to characterize mechanism of block produced by the compounds. Modifications, which preserve the flat structure of the tricyclic 9-aminoacridine moiety, affect blocking activity and kinetics but not the foot-in-the-door mechanism. On the contrary, disruption of the flat structure changes the mechanism of block to trapping. It is concluded that flat aromatic structure is one of the critical determinants of the action mechanism of 9-aminoacridine. (C) 2008 Elsevier Ireland Ltd. All rights reserved.
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