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Titolo:
Enhanced 5-HT metabolism and synthesis rate by the new selective r5-HT1B receptor antagonist, NAS-181 in the rat brain
Autore:
Stenfors, C; Yu, H; Ross, SB;
Indirizzi:
Astra Res Ctr AB, Preclin Res & Dev, S-15185 Sodertalje, Sweden Astra Res Ctr AB Sodertalje Sweden S-15185 v, S-15185 Sodertalje, Sweden
Titolo Testata:
NEUROPHARMACOLOGY
fascicolo: 4, volume: 39, anno: 2000,
pagine: 553 - 560
SICI:
0028-3908(2000)39:4<553:E5MASR>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
REUPTAKE INHIBITOR; FRONTAL-CORTEX; GUINEA-PIG; IN-VIVO; PHARMACOLOGICAL CHARACTERIZATION; BINDING-SITES; AUTORECEPTOR; ANPIRTOLINE; AGONIST; ACID;
Keywords:
r5-hydroxytryptamine(1B) receptors; NAS-181; anpirtoline; 5-HT metabolism; 5-HT synthesis; rat brain;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Stenfors, C Astra Res Ctr AB, Preclin Res & Dev, S-15185 Sodertalje, Sweden Astra Res Ctr AB Sodertalje Sweden S-15185 odertalje, Sweden
Citazione:
C. Stenfors et al., "Enhanced 5-HT metabolism and synthesis rate by the new selective r5-HT1B receptor antagonist, NAS-181 in the rat brain", NEUROPHARM, 39(4), 2000, pp. 553-560

Abstract

NAS-181 ((R)-(+)-2-(3-morpholinomethyl-2H-chromen-8-yl) oxymethyl-morpholine methanesulfonate) is a novel rat 5-hydroxytryptamine(1B),,, (r5-HT1B,,) receptor antagonist with high selectivity. The in vivo effects of NAS-181 on 5-HT metabolism and synthesis in the rat brain were examined. 5-HT metabolism, measured as the ratio 5-hydroxyindoleacetic acid (5-HIAA)/5-HT, was dose-dependently increased in all four brain regions analysed (hypothalamus,hippocampus, frontal cortex and striatum) at doses 0.1 to 20 mg/kg s.c. NAS-181. The enhancement of 5-HT metabolism at the dose 20 mg/kg s.c. was maximal one hour after the injection and was still significant eight hours butnot 24 hours after the injection. 5-HT synthesis rate measured as the accumulation of 5-hydroxytryptophan (5-HTP) after inhibition of the aromatic amino acid decarboxylase activity was also elevated by NAS-181 at doses 0.3 to 20 mg/kg s.c. NAS-181 competitively antagonised the decrease in 5-HT metabolism evoked by the r5-HT1B,, receptor agonist, anpirtoline, in hypothalamus, hippocampus and frontal cortex. Anpirtoline had no effect on 5-HT metabolism in striatum. However, anpirtoline antagonised the enhancement of 5-HTmetabolism induced by NAS-181 in striatum. Combined treatment of rats withNAS-181 and the 5-HT1A,, receptor antagonist, WAY-100635, increased 5-HT metabolism considerably more than when the compounds were given alone. (C) 2000 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/09/20 alle ore 22:54:42