文章基本信息

标题：Possible Existence of a Novel Receptor for Uridine Analogues in the Central Nervous System Using Two Isomers, N3-(S)-(+)- and N3-(R)-(−)-α-Hydroxy-β-phenethyluridines
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作者：Toshiyuki KIMURA ; Masaaki MIKI ; Michio IKEDA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2001
卷号：24
期号：6
页码：729-731
DOI：10.1248/bpb.24.729
出版社：The Pharmaceutical Society of Japan
摘要：Uridine analogue binding sites, the so-called uridine receptor, were observed in the experiments on specific [³H]N³-phenacyluridine binding to bovine synaptic membranes using two isomers, N³-(S)-(+)- and N³-(R)-(−)-α-hydroxy-β-phenethyluridine, as ligands. The potent hypnotic, N³-(S)-(+)-α-hydroxy-β-phenethyluridine, but not the (R)-isomer, strongly inhibited [³H]N³-phenacyluridine binding. The racemate had inhibitory activity intermediate between that of the two α-hydroxy-β-phenethyluridines ((R)- or (S)-isomers). The inhibitory constants of these compounds were determined. The K_i values of N³-phenacyluridine, α-hydroxy-β-phenethyluridine (racemate), N³-(R)-(−)-, and N³-(S)-(+)-α-hydroxy-β-phenethyluridine were 0.65, 397.4, 1908, and 10.2 nM, respectively. The present results indicate the existence of uridine receptors in the central nervous system in relation to their hypnotic activities reported previously.
关键词：N3-phenacyluridine;N3-(S)-(+)-α-hydroxy-β-phenethyluridine;uridine receptor;hypnotic;central nervous system;isomer