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Titolo:
Venlafaxine: Discrepancy between in vivo 5-HT and NE reuptake blockade andaffinity for reuptake sites
Autore:
Beique, JC; De Montigny, C; Blier, P; Debonnel, G;
Indirizzi:
McGillCanada Dept Psychiat, Neurobiol Psychiat Unit, Montreal, PQ H3A 1A1,McGill Univ Montreal PQ Canada H3A 1A1 ychiat Unit, Montreal, PQ H3A 1A1,
Titolo Testata:
SYNAPSE
fascicolo: 3, volume: 32, anno: 1999,
pagine: 198 - 211
SICI:
0887-4476(19990601)32:3<198:VDBIV5>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
SEROTONIN UPTAKE INHIBITORS; RAT LOCUS-COERULEUS; SPONTANEOUS FIRING RATE; H-3 PAROXETINE BINDING; DORSAL RAPHE NEURONS; MAJOR DEPRESSION; NORADRENERGIC NEURONS; ANTIDEPRESSANT DRUGS; IN-VIVO; NORADRENALINE UPTAKE;
Keywords:
antidepressant; dorsal raphe; locus coeruleus; paroxetine; desipramine; fenfluramine; tyramine; releaser;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
69
Recensione:
Indirizzi per estratti:
Indirizzo: Beique, JC McGillCanada Dept Psychiat, Neurobiol Psychiat Unit, Montreal, PQ H3A 1A1, McGill Univ Montreal PQ Canada H3A 1A1 , Montreal, PQ H3A 1A1,
Citazione:
J.C. Beique et al., "Venlafaxine: Discrepancy between in vivo 5-HT and NE reuptake blockade andaffinity for reuptake sites", SYNAPSE, 32(3), 1999, pp. 198-211

Abstract

Using an in vivo electrophysiological paradigm, venlafaxine and paroxetinedisplayed similar potency for suppressing the firing activity of dorsal raphe 5-HT neurons (ED50: 233 and 211 mu g/kg i.v., respectively), while venlafaxine was three times less potent than desipramine (ED50: 727 and 241 mu g/kg i.v., respectively) to suppress the firing activity of locus coeruleusNE neurons. The selective 5-HT1A receptor antagonist WAY 100635 (100 mu g/kg, i.v.) reversed the suppressant effect of venlafaxine and paroxetine on the firing activity of 5-HT neurons and the alpha(2)-adrenoceptor antagonist piperoxane (1 mg/kg, i.v.) reversed those of venlafaxine and desipramine on the firing activity of NE neurons. The ED50 Of venlafaxine on the firingactivity of 5-HT neurons was not altered (ED50: 264 pg/kg) in noradrenergic-lesioned rats, while the suppressant effect of venlafaxine on the firing activity of NE neurons was greater in serotonergic lesioned rats (ED50: 285pg/kg). Taken together, these results suggest that, in vivo, venlafaxine blocks both reuptake processes, its potency to block the 5-HT reuptake process being greater than that for NE. Since the affinities of venlafaxine for the 5-HT and NE reuptake carriers are not in keeping with its potencies forsuppressing the firing activity of 5-HT and NE neurons, the suppressant effect of venlafaxine on the firing activity of 5-HT and NE neurons observed in vivo may not be mediated solely by its action on the [H-3]cyanoimipramine and [H-3]nisoxetine binding sites. In an attempt to unravel the mechanismresponsible for this peculiarity, in vitro superfusion experiments were carried out in rat brain slices to assess a putative monoamine releasing property for venlafaxine. (+/-)Fenfluramine and tyramine substantially increased the spontaneous outflow of [H-3]5-HT and [H-3]NE, respectively, while venlafaxine was devoid of such releasing properties. (C) 1999 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 11:59:13