English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Plus monthly

Global: Zendy Tools annual

Global: Zendy Tools monthly

Global: Zendy Free Plan

The metabolism and hypnotic mechanism of N3-phenacyluridine were studied in mouse. Of the radioactivity, 65% was excreted in urine within 48 hours after i.p. administration of [3H]N3-phenacyluridine. The urinary metabolites N3-phenacyluracil and N3-α-hydroxy-β-phenethyluridine were excreted, isolated and analyzed by mass spectrometry. Racemates of N3-α-hydroxy-β-phenethyluridine were synthesized and both isomers were separated as N3-(S)-(+)- and N3-(R)-(-)-α-hydroxy-β-phenethyluridine by HPLC (CHIRALCEL-OJ column). The reduction process took place with high stereo-selectivity, which gave an alcohol product in the urine with same retention as one of the synthetic isomers separated by HPLC. N3-Phenacyluracil and uridine were identified as minor metabolites. N3-(S)-(+)-α-hydroxy-β-phenethyluridine, but not N3-(R)-(-)-α-hydroxy-β-phenethyluridine, possessed hypnotic activity in mice and potentiated pentobarbital-induced sleep with a similar potency to the parent compound, N3-phenacyluridine. An active metabolite, N3-(S)-(+)-α-hydroxy-β-phenethyluridine, inhibited [3H]N3-phenacyluridine binding to synaptic membrane of bovine thalamus showing 10.2 nM of Ki value, while N3-phenacyluridine, N3-(R)-(-)-α-hydroxy-β-phenethyluridine and racemate had 0.65, 397.4 and 1908 nM of Ki values, respectively. The present study indicates that N3-(S)-(+)-α-hydroxy-β-phenethyluridinea, major metabolite of N3-phenacyluridine, is an active metabolite and bound a novel uridine receptor involving the hypnotic activity.

yakubutsu dōtai

FINDING OF A NOVEL RECEPTOR FOR URIDINES USING TWO ENANTIOMER METABOLITES OF A NEW HYPNOTIC, N&lt;SUP&gt;3&lt;/SUP&gt;-PHENACYLURIDINE, ITS ACTION MECHANISM AND APPLICATION TO DEVELOPMENT OF DRUG