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Titolo:
COMPARISON OF THE EFFECTS OF SERTRALINE AND ITS METABOLITE DESMETHYLSERTRALINE ON BLOCKADE OF CENTRAL 5-HT REUPTAKE IN-VIVO
Autore:
SPROUSE J; CLARKE T; REYNOLDS L; HEYM J; ROLLEMA H;
Indirizzi:
PFIZER INC,DEPT NEUROSCI GROTON CT 06340
Titolo Testata:
Neuropsychopharmacology
fascicolo: 4, volume: 14, anno: 1996,
pagine: 225 - 231
SICI:
0893-133X(1996)14:4<225:COTEOS>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN; RAPHE NEURONS; INVIVO; 5-HYDROXYTRYPTAMINE; ANTIDEPRESSANT; MICRODIALYSIS; SEROTONIN; SYNAPTOSOMES; INHIBITION; RELEASE;
Keywords:
SELECTIVE SEROTONIN REUPTAKE INHIBITOR; SERTRALINE; DESMETHYLSERTRALINE; MICRODIALYSIS; ELECTROPHYSIOLOGY; DORSAL RAPHE NUCLEUS; STRIATUM;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Physical, Chemical & Earth Sciences
Physical, Chemical & Earth Sciences
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
25
Recensione:
Indirizzi per estratti:
Citazione:
J. Sprouse et al., "COMPARISON OF THE EFFECTS OF SERTRALINE AND ITS METABOLITE DESMETHYLSERTRALINE ON BLOCKADE OF CENTRAL 5-HT REUPTAKE IN-VIVO", Neuropsychopharmacology, 14(4), 1996, pp. 225-231

Abstract

N-demethylation of the selective serotonin reuptake inhibitor sertraline to desmethylsertraline yields a compound with 10- to 20-fold less potency at blocking serotonin (5-HT) reuptake as measured in vitro. Inthe present study desmethylsertraline (DMS) was examined in two in vivo models of reuptake inhibition-elevation of extracellular 5-HT in the corpus striatum as measured by microdilaysis and inhibition of firing of serotonin-containing dorsal raphe neurons. Whereas sertraline (1,3.2, and 10 mg/kg SC) produced a dose-dependent increase in extracellular 5-HT and a decrease in 5-HIAA in rat striatum, desmethylsertralinewas without effect on either parameter. In similar fashion, desmethylsertraline had no effect on dorsal raphe cell firing at a dose (1,000 mu g/kg IV) nearly 20-fold the ED(50) for sertraline (52 mu g/kg). Taken together, these data suggest that DMS does not contribute to the blockade of central 5-HT reuptake produced by sertraline in vivo and therefore would be expected to play a negligible role in its clinical activity.

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Documento generato il 05/12/20 alle ore 13:52:59