Binding affinity of N3-substituted uridine for synaptic membrane and their CNS depressant effects.
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.
Kimura
T
T
Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan.
Miki
M
M
Watanabe
K
K
Kondo
S
S
Ho
I K
IK
Yamamoto
I
I
D000818:Animals; D002417:Cattle; D002490:Central Nervous System / Q000187:drug effects*; D003864:Depression, Chemical; D006993:Hypnotics and Sedatives / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D066298:In Vitro Techniques; D011741:Pyrimidine Nucleosides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D011869:Radioligand Assay; D013329:Structure-Activity Relationship; D013570:Synaptic Membranes / Q000378:metabolism*; D014529:Uridine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology
D006993:Hypnotics and Sedatives; D011741:Pyrimidine Nucleosides; D014529:Uridine