(7S)-Kaitocephalin as a potent NMDA receptor selective ligand. Issue 4 (11th December 2015)

• Record Type: Journal Article
• Authors: Yasuno, Yoko; Hamada, Makoto; Kawasaki, Masanori; Shimamoto, Keiko; Shigeri, Yasushi; Akizawa, Toshifumi; Konishi, Motomi; Ohfune, Yasufumi; Shinada, Tetsuro
• Is Part Of: Organic & biomolecular chemistry. Volume 14:Issue 4(2016)
• Page Start: 1206
• Page End: 1210
• Publication Date: 2015-12-11
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c5ob02301g
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : A structure–activity relationship (SAR) study of kaitocephalin, known to be a potent naturally occurring NMDA receptor ligand, was performed. 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 (7 S )-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 (7 S )-KCP [ K i = 29 nM] was 3.7-fold less potent than that of KCP [ K i = 7.8 nM].