(7S)-Kaitocephalin as a potent NMDA receptor selective ligand†,10.1039/C5OB02301G

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

(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

Organic & Biomolecular Chemistry Pub Date : 12/01/2015 00:00:00 , DOI:10.1039/C5OB02301G

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 [K_i = 29 nM] was 3.7-fold less potent than that of KCP [K_i = 7.8 nM].