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].
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Dose-Response Relationship, Drug
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Eupenicillium / chemistry
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Ligands
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Molecular Conformation
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Pyrroles / chemical synthesis
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Rats
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Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
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Receptors, N-Methyl-D-Aspartate / metabolism*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Ligands
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Pyrroles
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Receptors, N-Methyl-D-Aspartate
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kaitocephalin