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. 2020 Dec 1;10(12):928. doi: 10.3390/brainsci10120928

Table 1.

NMDAR channel blockers and their effects on gating.

Compound Structure Type of Blocker Effects on Gating
Magnesium graphic file with name brainsci-10-00928-i001.jpg Unclear—due to fast unblocking kinetics, trapping of Mg2+ has not been directly demonstrated. None [13,202].
9-aminoacridine graphic file with name brainsci-10-00928-i002.jpg Sequential [7,201]. Stabilizes open state [7,201].
Prevents agonist dissociation [7,201].
IEM-1754 graphic file with name brainsci-10-00928-i003.jpg Depolarized potentials: sequential [173].
Strongly negative potentials: trapping [173].
Depolarized potentials: Stabilizes open state [173].
Amantadine graphic file with name brainsci-10-00928-i004.jpg Partial trapping [12,13]. Accelerates channel closure of native NMDARs and GluN1/2B receptors [8].
Memantine graphic file with name brainsci-10-00928-i005.jpg Partial trapping [8,16,197,203,204]. Slows GluN1/2A receptor recovery from Ca2+-dependent desensitization [3].
Ketamine graphic file with name brainsci-10-00928-i006.jpg Trapping [204]. Accelerates GluN1/2B receptor recovery from desensitization [3].

Magnesium is depicted coordinating six water molecules, and all organic blockers are depicted in bond-line format. Blockers structures are scaled to depict approximate relative sizes.