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Issue 4, 2016
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(7S)-Kaitocephalin as a potent NMDA receptor selective ligand

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A structure–activity relationship (SAR) study of kaitocephalin (KCP), known to be a potent naturally occurring NMDA receptor ligand, was performed. This study led us to the discovery of (7S)-kaitocephalin as a highly selective NMDA receptor ligand. It displayed a 22-fold higher degree of selectivity for the NMDA receptor over KCP, though the binding affinity of (7S)-KCP [Ki = 29 nM] was 3.7-fold less potent than that of KCP [Ki = 7.8 nM].

Graphical abstract: (7S)-Kaitocephalin as a potent NMDA receptor selective ligand

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The article was received on 09 Nov 2015, accepted on 30 Nov 2015 and first published on 01 Dec 2015

Article type: Communication
DOI: 10.1039/C5OB02301G
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Org. Biomol. Chem., 2016,14, 1206-1210

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    (7S)-Kaitocephalin as a potent NMDA receptor selective ligand

    Y. Yasuno, M. Hamada, M. Kawasaki, K. Shimamoto, Y. Shigeri, T. Akizawa, M. Konishi, Y. Ohfune and T. Shinada, Org. Biomol. Chem., 2016, 14, 1206
    DOI: 10.1039/C5OB02301G

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