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

Yoko Yasuno, Makoto Hamada, Masanori Kawasaki, Keiko Shimamoto, Yasushi Shigeri, Toshifumi Akizawa, Motomi Konishi, Yasufumi Ohfune, Tetsuro Shinada

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

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].

Original languageEnglish
Pages (from-to)1206-1210
Number of pages5
JournalOrganic and Biomolecular Chemistry
Volume14
Issue number4
DOIs
Publication statusPublished - Jan 1 2016
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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  • Cite this

    Yasuno, Y., Hamada, M., Kawasaki, M., Shimamoto, K., Shigeri, Y., Akizawa, T., Konishi, M., Ohfune, Y., & Shinada, T. (2016). (7S)-Kaitocephalin as a potent NMDA receptor selective ligand. Organic and Biomolecular Chemistry, 14(4), 1206-1210. https://doi.org/10.1039/c5ob02301g