Aromatic analogs of arcaine inhibit MK-801 binding to the NMDA receptor.
Aromatic analogs of arcaine inhibit MK-801 binding to the NMDA receptor.
复制标题
阿卡因的芳香类似物抑制 MK-801 与 NMDA 受体的结合。
DOI：
10.1016/s0960-894x(98)00631-3
复制
发表时间：
1998
影响因子：
2.7
通讯作者：
Hamilton,AD
中科院分区：
文献类型：
--
作者：
Sharma,TA;Carr,AJ;Davis,RS;Reynolds,IJ;Hamilton,AD
Aromatic analogs of arcaine were shown to have inhibitory effects on the binding of the channel blocking drug [3H]MK-801 to the NMDA receptor complex. The most potent compound of the series was an N,N′-bis(propyl)guanidinium which inhibited [3H]MK-801 binding with an IC50of 0.58 μM and an IC50of 12.17 μM upon addition of 100 μM spermidine. The increase in IC50upon addition of spermidine suggests competitive antagonism between the inhibitor and spermidine at the arcaine-sensitive polyamine site of the NMDA receptor complex.
