(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 journalArticlepeer-review

6 Citations (Scopus)


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
Issue number4
Publication statusPublished - 2016
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry


Dive into the research topics of '(7S)-Kaitocephalin as a potent NMDA receptor selective ligand'. Together they form a unique fingerprint.

Cite this