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Titolo:
DISTINCT EFFECTS OF IMIPRAMINE ON 5-HYDROXYTRYPTAMINE UPTAKE MEDIATEDBY THE RECOMBINANT RAT SEROTONIN TRANSPORTER SERT1
Autore:
SUR C; BETZ H; SCHLOSS P;
Indirizzi:
MAX PLANCK INST BRAIN RES,DEPT NEUROCHEM,DEUTSCHORDENSTR 46 D-60528 FRANKFURT GERMANY MAX PLANCK INST BRAIN RES,DEPT NEUROCHEM D-60528 FRANKFURT GERMANY
Titolo Testata:
Journal of neurochemistry
fascicolo: 6, volume: 70, anno: 1998,
pagine: 2545 - 2553
SICI:
0022-3042(1998)70:6<2545:DEOIO5>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
)H-3>IMIPRAMINE BINDING; ALLOSTERIC INTERACTION; HUMAN-PLATELETS; REUPTAKE INHIBITORS; LIGAND-BINDING; ION DEPENDENCE; HIGH-AFFINITY; EXPRESSION; CLONING; KINETICS;
Keywords:
SEROTONIN; UPTAKE; ANTIDEPRESSANT BINDING; TRICYCLIC ANTIDEPRESSANTS; SELECTIVE SEROTONIN UPTAKE INHIBITORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
32
Recensione:
Indirizzi per estratti:
Citazione:
C. Sur et al., "DISTINCT EFFECTS OF IMIPRAMINE ON 5-HYDROXYTRYPTAMINE UPTAKE MEDIATEDBY THE RECOMBINANT RAT SEROTONIN TRANSPORTER SERT1", Journal of neurochemistry, 70(6), 1998, pp. 2545-2553

Abstract

Tricyclic and nontricyclic serotonin [5-hydroxytryptamine (5-HT)] uptake inhibitors are widely used for the treatment of depression. Here, we show that both the tricyclic antidepressant imipramine and the nontricyclic antidepressant citalopram competitively inhibit 5-HT transport mediated by the recombinant rat 5-HT transporter SERT1. For citalopram, the concentration producing half-maximal transport inhibition was in the same order of magnitude as its K-D value determined by equilibrium binding. In contrast, the inhibitory potency of imipramine was more than one order of magnitude lower than its K-D value. Our data are consistent with low-affinity imipramine binding occurring at or close to the substrate recognition site, which also binds citalopram. Occupation of the high-affinity imipramine binding site on SERT1 did not affect 5-HT transport but allosterically displaced citalopram from the substrate recognition site. Consequently, low concentrations of imipramine partially protected 5-HT transport from citalopram inhibition. This protection was only observed in the presence of Na+ because high-affinity imipramine binding is strictly sodium-dependent. Thus, depending on which of its binding sites on SERT1 is occupied, imipramine may exert distinct effects on 5-HT uptake mediated by the recombinant rat 5-HTtransporter.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 09:14:31