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Titolo:
D-2 and 5HT(2A) receptor occupancy of different doses of quetiapine in schizophrenia: a PET study
Autore:
Gefvert, O; Lundberg, T; Wieselgren, IM; Bergstrom, M; Langstrom, B; Wiesel, FA; Lindstrom, L;
Indirizzi:
Cent Hosp, Dept Psychiat Res, S-72189 Vasteras, Sweden Cent Hosp Vasteras Sweden S-72189 Psychiat Res, S-72189 Vasteras, Sweden Uppsala Univ, Dept Neurosci, Uppsala, Sweden Uppsala Univ Uppsala Sweden ppsala Univ, Dept Neurosci, Uppsala, Sweden Uppsala Univ, PET Ctr, Uppsala, Sweden Uppsala Univ Uppsala SwedenUppsala Univ, PET Ctr, Uppsala, Sweden
Titolo Testata:
EUROPEAN NEUROPSYCHOPHARMACOLOGY
fascicolo: 2, volume: 11, anno: 2001,
pagine: 105 - 110
SICI:
0924-977X(200104)11:2<105:DA5ROO>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON-EMISSION-TOMOGRAPHY; ANTIPSYCHOTIC-DRUGS; C-11 RACLOPRIDE; TIME-COURSE; CLOZAPINE; DOPAMINE; BRAIN; RISPERIDONE; HALOPERIDOL; OLANZAPINE;
Keywords:
quetiapine; schizophrenic; patients; PET; dopamine D-2 receptors; serotonin 5HT(2A) receptors; atypical antipsychotic;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
33
Recensione:
Indirizzi per estratti:
Indirizzo: Gefvert, O Cent Hosp, Dept Psychiat Res, S-72189 Vasteras, Sweden Cent Hosp Vasteras Sweden S-72189 s, S-72189 Vasteras, Sweden
Citazione:
O. Gefvert et al., "D-2 and 5HT(2A) receptor occupancy of different doses of quetiapine in schizophrenia: a PET study", EUR NEUROPS, 11(2), 2001, pp. 105-110

Abstract

Objective: Quetiapine is a novel antipsychotic agent with many atypical features, including low D-2 and higher 5HT(2A) affinity in vitro, low propensity to induce extra-pyramidal side effects and minimal effects on prolactinlevels. The purpose of this study was to investigate, using position emission tomography (PET), the relationship between plasma concentrations of different doses of quetiapine and occupancy of D-2 and 5HT(2A) receptors in schizophrenic patients, Methods: Five patients were treated with quetiapine (titrated to 750 or 450 mg/day) for 28 days, subsequently reduced weekly in a descending-dose schedule. Dopamine D-2 and 5HT(2A) occupancies were determined using [C-11] raclopride and [C-11] N-methylspiperone as ligands, respectively, and PET imaging. Results: Mean D, receptor occupancies of 41 and 30%, were observed at quetiapine doses of 750 and 450 mg/day. At lower doselevels no occupancy could be determined. Quetiapine: induced a consistently higher degree of 5HT(2A) receptor occupancy, with mean occupancies of 74 and 57% at doses of 750 anti 450 mg/day, respectively. No EPS emerged during the trial and most of the pre-trial EPS resolved during the study. Conclusions: In clinically effective doses, quetiapine induced low occupancy at D-2 receptors, which is consistent with atypical antipsychotics such as clozapine. and probably explains the lack of EPS observed in this trial. Correlations between receptor occupancy and plasma concentrations of quetiapine could not he calculated, although receptor occupancy increased with higher plasma concentrations for the 450 and 750 mg doses. (C) 2001 Elsevier Science B.V. All rights reserved.

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Documento generato il 19/01/20 alle ore 08:53:52