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  • 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
  • 本地全文:下载
  • 作者:Toshiyuki KIMURA ; Masaaki MIKI ; Michio IKEDA
  • 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 Ki 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
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