Desensitization Increase As an Additional Mode of Action for NMDA Receptor Open Channel Blockers

摘要

NMDA receptor channel blockers have differentmechanisms of interaction with ion channels. "Trap-ping blockers" remain within ion channel having noinfluence on gating process. Others, "foot-in-the-doorblockers", interfere with gating mechanism, preventingagonist to dissociate while blocker is inside the chan-nel. In the latter case channel blockade compete withdesensitization according to the kinetic scheme. Thusblocking mechanism has apparent influence on desen-sitization, which could mask real influence on desensi-tization.