Contreras P C, Bremer M E, Gray N M
CNS Diseases Research, G.D. Searle & Co., St. Louis, MO 63198.
Neurosci Lett. 1990 Aug 14;116(1-2):190-3. doi: 10.1016/0304-3940(90)90408-2.
SL 82.0715 and ifenprodil are potent anti-ischemic agents, which are believed to be due to non-competitive antagonism of N-methyl-D-aspartate (NMDA). It has been proposed that SL 82.0715 and ifenprodil non-competitively antagonize the actions of NMDA by interacting as antagonists with a polyamine site associated with the NMDA/phencyclidine (PCP)/glycine complex. The present study demonstrates that the actions of SL 82.0715 and ifenprodil may also be due in part to an interaction with sigma binding sites, a property that is not shared with polyamines.
SL 82.0715和ifenprodil是强效抗缺血药物，据信这是由于它们对N-甲基-D-天冬氨酸（NMDA）的非竞争性拮抗作用。有人提出，SL 82.0715和ifenprodil通过作为拮抗剂与与NMDA/苯环己哌啶（PCP）/甘氨酸复合物相关的多胺位点相互作用，从而非竞争性地拮抗NMDA的作用。本研究表明，SL 82.0715和ifenprodil的作用也可能部分归因于与σ结合位点的相互作用，而这是多胺所不具备的特性。
