Article

Dapsone analogs as potential polyamine binding site modulators of the N‐methyl‐D‐aspartate receptor complex

Drug Development Research (impact factor: 1.19). 02/2001; 51(4):268 - 272. DOI:10.1002/ddr.8 pp.268 - 272

ABSTRACT A high-throughput radioligand binding assay was used to screen a series of dapsone analogs for their capacity to displace [3H]-spermidine and [3H]-MK-801 from their respective binding sites on the N-methyl-D-aspartate (NMDA) receptor complex in rat brain homogenates. Dapsone did not alter [3H]-spermidine or [3H]-MK-801 binding, suggesting that the neuroprotective properties that have been attributed to this compound may not be due to modulation of the NMDA receptor complex at the polyamine binding site. In contrast, structural analogs of dapsone, including N-phenyl-1,4-phenyldiamine and 4,4′diaminoazobenzene, effectively displaced [3H]-SPD and [3H]-MK-801. These active dapsone analogs may represent a new class of polyamine binding site ligands that may provide opportunities for the rational design of novel NMDA receptor modulators. Drug Dev. Res. 51:268–272, 2000. © 2001 Wiley-Liss, Inc.

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Keywords

active dapsone analogs
 
dapsone
 
dapsone analogs
 
displace [3H]-spermidine
 
high-throughput radioligand binding assay
 
Inc
 
new class
 
NMDA
 
NMDA receptor complex
 
novel NMDA receptor modulators
 
polyamine binding site
 
polyamine binding site ligands
 
rat brain homogenates
 
rational design
 
respective binding sites
 
structural analogs