Abstract
The actions of the σ receptor ligand L-687,384 were studied on N- methyl- d - aspartate (NMDA)-induced currents recorded from outside-out patches obtained from cultured rat hippocampal pyramidal neurons and on NMDA-evoked rises in [Ca 2+] i in the same preparation. L-687,384 did not change the magnitudes of unitary NMDA currents or frequency of channel-openings but diminished channel-open probability by decreasing mean open time. This action was consistent with a voltage-dependent open-channel block of the NMDA channel by L-687,384 with a blocking rate constant of 5.9 × 10 6 M −1s −1 at −80 mV. L-687,384 also reduced NMDA-evoked rises in [Ca 2+] i in Fura-2-loaded neurons with an apparent IC 50 value of 49±8 μM. The results demonstrate that L-687,384 acts as an antagonist at the NMDA receptor-channel complex.
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