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Titolo:
BLOCKADE OF THE SEROTONIN AND NOREPINEPHRINE UPTAKE PROCESSES BY DULOXETINE - IN-VITRO AND IN-VIVO STUDIES IN THE RAT-BRAIN
Autore:
KASAMO K; BLIER P; DEMONTIGNY C;
Indirizzi:
MCGILL UNIV,DEPT PSYCHIAT,NEUROBIOL PSYCHIAT UNIT,1033 PINE AVE W MONTREAL PQ H3A 1A1 CANADA MCGILL UNIV,DEPT PSYCHIAT,NEUROBIOL PSYCHIAT UNIT MONTREAL PQ H3A 1A1CANADA
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 1, volume: 277, anno: 1996,
pagine: 278 - 286
SICI:
0022-3565(1996)277:1<278:BOTSAN>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
DORSAL RAPHE NEURONS; LOCUS COERULEUS; 5-HT AUTORECEPTORS; SINGLE-CELL; RECEPTORS; SENSITIVITY; HIPPOCAMPUS; INNERVATION; NUCLEI; ALPHA-2-ADRENOCEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
42
Recensione:
Indirizzi per estratti:
Citazione:
K. Kasamo et al., "BLOCKADE OF THE SEROTONIN AND NOREPINEPHRINE UPTAKE PROCESSES BY DULOXETINE - IN-VITRO AND IN-VIVO STUDIES IN THE RAT-BRAIN", The Journal of pharmacology and experimental therapeutics, 277(1), 1996, pp. 278-286

Abstract

In in vitro uptake experiments, duloxetine inhibited [H-3]5-hydroxytryptamine (5-HT) and [H-3]norepinephrine (NE) uptake in hippocampus slices of control rats with IC50 values of 28 and 46 nM, respectively. The uptake of both [H-3]5-HT and-[H-3]NE was equipotently inhibited in hippocampus slices prepared from rats treated for 2 days with differentdoses of duloxetine (5, 10, 15 and 20 mg/kg/day s.c.). In in vivo electrophysiological experiments in the hippocampus, the effects of duloxetine on the suppression of CA(3) pyramidal neuronal firing activity by microiontophoretically applied 5-HT and NE were examined with two modes of administration. Five successive i.v. injections (2 mg/kg each) significantly and dose-dependently prolonged the recovery time of the firing activity of hippocampus CA(3) pyramidal neurons from the 5-HT applications. A 2-day treatment (10, 15 and 20 mg/kg/day s.c.) also increased the recovery time in a dose-dependent manner. Whereas the recovery time from NE applications was unaffected by low doses of duloxetine (2 mg/kg i.v.; 10 mg/kg/day for 2 days), it was prolonged significantly by higher doses (8 and 10 mg/kg i.v.; 20 mg/kg/day for 2 days). Acute i.v. injections of duloxetine suppressed the spontaneous firing activity of dorsal raphe 5-HT and locus ceruleus NE neurons with ED(50) values of 99 and 475 mu g/kg, respectively. Taken together, the present results confirmed that duloxetine is a dual 5-HT/NE uptake inhibitor. Furthermore, the results obtained in in vivo experiments indicate that duloxetine has a preferential inhibitory effect on the 5-HT transporter.

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Documento generato il 03/06/20 alle ore 09:42:10