Molecular rearrangements of the extracellular vestibule in NMDAR channels during gating.

Abstract excerpt

Many N-methyl-D-aspartate receptor (NMDAR) channel blockers that have therapeutic potential can be trapped in the closed state. Using a combination of the substituted cysteine accessibility method and open channel blockers, we found that the M3 segment forms the core of the extracellular vestibule, including a deep site for trapping blockers. The M3 segment, as well as more superficial parts of the extracellular...

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• Central Nervous System
• Drug Interactions
• Excitatory Amino Acid Antagonists
• Extracellular Space
• Ion Channel Gating