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Titolo:
S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine
Autore:
Millan, MJ; Gobert, A; Lejeune, F; Newman-Tancredi, A; Rivet, JM; Auclair, A; Peglion, JL;
Indirizzi:
Inst Rech Servier, Ctr Rech Croissy, Dept Psychopharmacol, Paris, France Inst Rech Servier Paris France ssy, Dept Psychopharmacol, Paris, France Inst Rech Servier, Ctr Rech Suresnes, Med Chem Dept B, Paris, France Inst Rech Servier Paris France Suresnes, Med Chem Dept B, Paris, France
Titolo Testata:
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
fascicolo: 2, volume: 298, anno: 2001,
pagine: 565 - 580
SICI:
0022-3565(200108)298:2<565:SANLAB>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
REUPTAKE INHIBITOR VENLAFAXINE; RAT-BRAIN; ANTIDEPRESSANT ACTIVITY; EXTRACELLULAR DOPAMINE; MAJOR DEPRESSION; DOWN-REGULATION; FRONTAL-CORTEX; NORADRENALINE; FLUOXETINE; MODULATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
63
Recensione:
Indirizzi per estratti:
Indirizzo: Millan, MJ Inst Rech Servier, Ctr Rech Croissy, Dept Psychopharmacol, 125 Chemin Ronde, F-78290 Croissy Seine, France Inst Rech Servier 125 Chemin Ronde Croissy Seine France F-78290
Citazione:
M.J. Millan et al., "S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine", J PHARM EXP, 298(2), 2001, pp. 565-580

Abstract

S33005 displayed marked affinity for native, rat, and cloned human serotonin (5-HT) transporters (SERT) and less pronounced affinity for norepinephrine (NE) transporters (NET), while its affinity at dopamine (DA) transporters and >50 other sites was negligible. Reuptake of 5-HT and (less potently) NE into cerebral synaptosomes was inhibited by S33005, whereas DA reuptake was little affected. In vivo, S33005 prevented depletion of cerebral pools of 5-HT by parachloroamphetamine. Furthermore, it decreased electrical activity of raphe-localized serotonergic neurones, an action abolished by the 5-HT1A antagonist WAY100,635. At higher doses, S33005 blocked firing of locus ceruleus-localized adrenergic neurones, an action abolished by the alpha (2)-adrenergic antagonist idazoxan. In contrast, S33005 did not inhibit ventrotegmental dopaminergic neurones. In frontal cortex of freely moving rats, S33005 dose dependently elevated dialysate levels of 5-HT, NE, and DA. Inhippocampus, levels of 5-HT and NE were similarly elevated, while in nucleus accumbens and striatum, levels of 5-HT were increased whereas DA was unaffected. Upon chronic (2 weeks) administration, basal levels of NE were elevated in frontal cortex and, therein, 5-HT2A receptor density was decreased. Comparative studies with clinically used antidepressants showed that venlafaxine possessed a profile similar to S33005 but was less potent. Clomipramine likewise interacted with SERTs and NETs but also with several other receptors types, while citalopram and reboxetine were preferential ligands ofSERTs and NETs, respectively. In conclusion, S33005 interacts potently with SERTs and, less markedly, with NETS. It enhances extracellular levels of 5-HT and NE throughout corticolimbic structures and selectively elevates dialysis levels of DA in frontal cortex versus subcortical regions.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 13:59:08