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Titolo:
Possible existence of a novel receptor for uridine analogues in the central nervous system using two isomers, N-3-(S)-(+)- and N-3-(R)-(-)-alpha-hydroxy-beta-phenethyluridines
Autore:
Kimura, T; Miki, M; Ikeda, M; Yonemoto, S; Watanabe, K; Kondo, S; Ho, IK; Yamamoto, I;
Indirizzi:
Hokuriku Univ, Fac Pharmaceut Sci, Dept Hyg Chem, Kanazawa, Ishikawa 9201181, Japan Hokuriku Univ Kanazawa Ishikawa Japan 9201181 wa, Ishikawa 9201181, Japan Nissui Pharmaceut Co Ltd, Ibaraki, Osaka 3070036, Japan Nissui Pharmaceut Co Ltd Ibaraki Osaka Japan 3070036 Osaka 3070036, Japan Univ Mississippi, Med Ctr, Dept Pharmacol & Toxicol, Jackson, MS 39216 USAUniv Mississippi Jackson MS USA 39216 ol & Toxicol, Jackson, MS 39216 USA
Titolo Testata:
BIOLOGICAL & PHARMACEUTICAL BULLETIN
fascicolo: 6, volume: 24, anno: 2001,
pagine: 729 - 731
SICI:
0918-6158(200106)24:6<729:PEOANR>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
HYPNOTIC ACTIVITY; N-3-PHENACYLURIDINE; MICE; DEPRESSANT; BINDING; SITES; MOUSE; RATS;
Keywords:
N-3-phenacyluridine; N-3-(S)-(+)-(alpha-hydroxy-beta-phenethyluridine; uridine receptor; hypnotic; central nervous system; isomer;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: Yamamoto, I Hokuriku Univ, Fac Pharmaceut Sci, Dept Hyg Chem, Ho-3, Kanazawa, Ishikawa9201181, Japan Hokuriku Univ Ho-3 Kanazawa Ishikawa Japan 9201181 1181, Japan
Citazione:
T. Kimura et al., "Possible existence of a novel receptor for uridine analogues in the central nervous system using two isomers, N-3-(S)-(+)- and N-3-(R)-(-)-alpha-hydroxy-beta-phenethyluridines", BIOL PHAR B, 24(6), 2001, pp. 729-731

Abstract

Uridine analogue binding sites, the so-called uridine receptor, were observed in the experiments on specific [H-3]N-3-phenacyluridine binding to bovine synaptic membranes using two isomers, N-3-(S)-(+)- and N-3-(R)-(-)-alpha-hydroxy-beta -phenethyluridine, as ligands. The potent hypnotic, N-3-(S)-(+)-alpha -hydroxy-beta -phenethyluridine, but not the (R)-isomer, stronglyinhibited [H-3]N-3-phenacyluridine binding. The racemate had inhibitory activity intermediate between that of the two alpha -hydroxy-beta -phenethyluridines ((R)- or (S)-isomers). The inhibitory constants of these compounds were determined. The Ki values of N3-phenacyluridine, alpha -hydroxy-beta -phenethyluridine (racemate), N-3-(R)-(-)-, and N-3-O-(+)-alpha -hydroxy-beta -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.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 03:54:35