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Titolo:
AUTORADIOGRAPHIC CHARACTERIZATION OF BINDING-SITES FOR [H-3] MILNACIPRAN, A NEW ANTIDEPRESSANT DRUG, AND THEIR RELATIONSHIP TO THE SEROTONIN TRANSPORTER IN RAT-BRAIN
Autore:
BARONE P; MORET C; BRILEY M; FILLION G;
Indirizzi:
INST PASTEUR,NIE,PHARMACOL LAB,28 RUE DR ROUX F-75724 PARIS 15 FRANCE CTR RECH PIERRE FABRE F-81106 CASTRES FRANCE
Titolo Testata:
Brain research
fascicolo: 1-2, volume: 668, anno: 1994,
pagine: 129 - 143
SICI:
0006-8993(1994)668:1-2<129:ACOBF[>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
QUANTITATIVE AUTORADIOGRAPHY; H-3 PAROXETINE; 5-HYDROXYTRYPTAMINE UPTAKE; )IMIPRAMINE-H-3 BINDING; )H-3>IMIPRAMINE BINDING; NOREPINEPHRINE UPTAKE; REGIONAL DISTRIBUTION; POTENT INHIBITOR; LOCALIZATION; CLONING;
Keywords:
MILNACIPRAN; PAROXETINE; ANTIDEPRESSANT BINDING SITES; SEROTONIN TRANSPORTER; AUTORADIOGRAPHY; LESION; 5,7-DIHYDROXYTRYPTAMINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
41
Recensione:
Indirizzi per estratti:
Citazione:
P. Barone et al., "AUTORADIOGRAPHIC CHARACTERIZATION OF BINDING-SITES FOR [H-3] MILNACIPRAN, A NEW ANTIDEPRESSANT DRUG, AND THEIR RELATIONSHIP TO THE SEROTONIN TRANSPORTER IN RAT-BRAIN", Brain research, 668(1-2), 1994, pp. 129-143

Abstract

Milnacipran is a new antidepressant drug and an equipotent inhibitor of the uptake of serotonin and noradrenaline, Quantitative autoradiography and radioligand binding studies were used to characterize recognition sites of [H-3]milnacipran in rat brain. [H-3]Milnacipran demonstrated saturable, reversible and nanomolar affinity binding. The bindingwas Na+-dependent, potently displaced by serotonin uptake inhibitors in all structures and moderately or weakly displaced by catecholamine uptake inhibitors (order of potency: paroxetine > fluoxetine > mazindol > desipramine > nomifensine > maprotiline). High density of recognition sites were found in structures dense in serotonergic innervation (raphe, basal ganglia, colliculi, cortex). The autoradiographic patternof [H-3]milnacipran recognition sites resembled that of [H-3]paroxetine, but their distribution did not correlate well in some structures. Selective lesioning of serotonergic neurons by intracerebral injectionof 5,7-dihydroxytryptamine caused a large decrease of [H-3]milnacipran binding in various regions (septum, caudate, hippocampus, thalamus, ventral and dorsal hypothalamus), but in other structures, the [H-3]milnacipran binding was partially affected (putamen) or even unchanged (amygdala, lateral hypothalamus). In contrast, lesion of noradrenergic neurons by intraperitoneal administration of [N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine] did not affect the binding of [H-3]milnacipran in any region. These results show that [H-3]mxilnacipran mainly binds to the serotonin transporter and does not recognize the catecholamine transporters under the conditions used, In addition, [H-3]milnacipran might also bind to other sites, serotonin transporter localized on non-serotonergic neurons or serotonergic neurons insensitive to 5,7-DHT neurotoxicity.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 12/07/20 alle ore 06:51:10