Aromatic analogs of arcaine inhibit MK-801 binding to the NMDA receptor

[摘要] Aromatic analogs of arcaine were shown to have inhibitory effects on the binding of the channel blocking drug [H-3]MK-801 to the NMDA receptor complex. The most potent compound of the series was an N,N'-bis(propyl)guanidinium which inhibited [H-3]MK-801 binding with an IC50 of 0.58 mu M and an IC50 of 12.17 mu M upon addition of 100 mu M spermidine. The increase in IC50 upon addition of spermidine suggests competitive antagonism between the inhibitor and spermidine at the arcaine-sensitive polyamine site of the NMDA receptor complex. (C) 1998 Published by Elsevier Science Ltd. All rights reserved.

[发布日期] 1998-12-15