Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 14, Issue 4, Pages 1206-1210Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ob02301g
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Funding
- Scientific Research of Innovative Areas, Chemical Biology of Natural Products, the Ministry of Education, Culture, Sports, Science and Technology [23102009]
- Japan Society for the Promotion of Science [23228001, 25282233]
- Japan Science Society
- Grants-in-Aid for Scientific Research [23102009, 25282233] Funding Source: KAKEN
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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)-kaito-cephalin 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].
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