Possible Existence of a Novel Receptor for Uridine Analogues in the Central Nervous System Using Two Isomers, N^3-(S)-(+)-and N^3-(R)-(-)-α-Hydroxy-β-phenethyluridines

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Uridine analogue binding sites, the so-called uridine receptor, were observed in the experiments on specific [^3N]N^3-phenacyl-uridine binding to bovine synapti membranes using two isomers, N^3-(S)-(+)- and N^3-(R)-(-)-α-hydroxy-β-phenethyluridine, as ligands. The potent hypnitic, N^3-(S)-(+)-α-hydroxy-β-phenethyluridine, but not the (R)-isomer, strongle inhibited [^3H]N^3-phenacyluridine binding. The racemate had inhibirory 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 N^3-phenacyluidine, α-hydroxy-β-phenethyluridine(racemate), N^3-(R)-(-)-, and N^3-(S)-(+)-α-hydroxy-β-phenethyluridine were 0.65, 397.4, 1908, and 10.2n_M, respectively. The present results indicate the existence of uridine receptors in the central nervous system in relation to their hypnotic activities reported previously.
社団法人日本薬学会の論文
2001-06-01