title: (7S)-Kaitocephalin as a potent NMDA receptor selective ligand.
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].
authors.affiliation: Graduate School of Science, Osaka City University, 3-3-138, Sugimoto, Sumiyoshi, Osaka 558-8585, Japan. shinada@sci.osaka-cu.ac.jp.
authors.forename: Yoko
authors.initials: Y
authors.lastname: Yasuno
authors.forename: Makoto
authors.initials: M
authors.lastname: Hamada
authors.forename: Masanori
authors.initials: M
authors.lastname: Kawasaki
authors.forename: Keiko
authors.initials: K
authors.lastname: Shimamoto
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Shigeri
authors.forename: Toshifumi
authors.initials: T
authors.lastname: Akizawa
authors.forename: Motomi
authors.initials: M
authors.lastname: Konishi
authors.forename: Yasufumi
authors.initials: Y
authors.lastname: Ohfune
authors.forename: Tetsuro
authors.initials: T
authors.lastname: Shinada
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D055324:Eupenicillium / Q000737:chemistry; D008024:Ligands; D008968:Molecular Conformation; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D011758:Pyrroles; D016194:Receptors, N-Methyl-D-Aspartate; C442421:kaitocephalin