Kimura T, Miki M, Watanabe K, Kondo S, Ho I K, Yamamoto I
Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan.
Nucleic Acids Symp Ser. 1995(34):147-8.
The binding affinity for synaptic membrane from bovine thalamus of N3-phenacyl substituted pyrimidine nucleosides having CNS depressant activity was examined by radio receptor assay. N3-Phenacyl derivatives of uridine, thymidine, deoxyuridine, 6-azauridine and arabinofuranosyluracil inhibited specific [3H]uridine binding and exhibited hypnotic activity. However, N3-phenacyl-2',3'-O-isopropylideneuridine, of which structure was different from sugar moiety of N3-phenacyluridine, showed neither the binding affinity nor the hypnotic activity. The results indicated that CNS depressant effect of pyrimidine nucleoside derivatives might relate to uridine binding affinity, so called uridine receptor.
通过放射受体分析法检测了具有中枢神经系统抑制活性的 N3-苯甲酰基取代嘧啶核苷对牛丘脑突触膜的结合亲和力。尿苷、胸苷、脱氧尿苷、6-氮杂尿苷和阿拉伯呋喃糖基尿嘧啶的 N3-苯甲酰基衍生物抑制特异性[3H]尿苷结合并表现出催眠活性。然而，结构与 N3-苯甲酰基尿苷糖部分不同的 N3-苯甲酰基-2',3'-O-异丙叉基尿苷既没有结合亲和力也没有催眠活性。结果表明嘧啶核苷衍生物的中枢神经系统抑制作用可能与尿苷结合亲和力有关，即所谓的尿苷受体。
