Article
Structural analysis of the positive AMPA receptor modulators CX516 and Me-CX516 in complex with the GluA2 ligand-binding domain.
Acta crystallographica. Section D, Biological crystallography - 1 Sept 2013
Krintel Christian, Harpsøe Kasper, Zachariassen Linda G, Peters Dan, Frydenvang Karla, Pickering Darryl S, Gajhede Michael, Kastrup Jette S
Abstract excerpt
Positive allosteric modulators of the ionotropic glutamate receptor A2 (GluA2) can serve as lead compounds for the development of cognitive enhancers. Several benzamide-type (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor modulators such as aniracetam, CX516 and CX614 have been shown to inhibit the deactivation of AMPA receptors with a less pronounced effect on desensitization....
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