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Titolo:
N-[C-11]METHYLSPIPERONE PET, IN CONTRAST TO [C-11] RACLOPRIDE, FAILS TO DETECT D-2 RECEPTOR OCCUPANCY BY AN ATYPICAL NEUROLEPTIC
Autore:
HAGBERG G; GEFVERT O; BERGSTROM M; WIESELGREN IM; LINDSTROM L; WIESEL FA; LANGSTROM B;
Indirizzi:
UNIV UPPSALA HOSP,PET CTR S-75185 UPPSALA SWEDEN UPPSALA UNIV,DEPT PSYCHIAT RES,VASTERAS CENT HOSP S-72189 VASTERAS SWEDEN UNIV UPPSALA HOSP,DEPT PSYCHIAT S-75017 UPPSALA SWEDEN UPPSALA UNIV,PET CTR UPPSALA SWEDEN
Titolo Testata:
PSYCHIATRY RESEARCH-NEUROIMAGING
fascicolo: 3, volume: 82, anno: 1998,
pagine: 147 - 160
SICI:
0925-4927(1998)82:3<147:NPICT[>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; NAIVE SCHIZOPHRENIC-PATIENTS; C-11 RACLOPRIDE BINDING; D2 DOPAMINE-RECEPTORS; H-3 N-METHYLSPIPERONE; HUMAN-BRAIN; SEROTONIN RECEPTORS; ANTIPSYCHOTIC-DRUGS; KINETIC-ANALYSIS; INVIVO BINDING;
Keywords:
POSITRON EMISSION TOMOGRAPHY; [C-11] RACLOPRIDE; N-[C-11]METHYLSPIPERONE; QUETIAPINE; SCHIZOPHRENIA; DOPAMINE RECEPTORS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
49
Recensione:
Indirizzi per estratti:
Citazione:
G. Hagberg et al., "N-[C-11]METHYLSPIPERONE PET, IN CONTRAST TO [C-11] RACLOPRIDE, FAILS TO DETECT D-2 RECEPTOR OCCUPANCY BY AN ATYPICAL NEUROLEPTIC", PSYCHIATRY RESEARCH-NEUROIMAGING, 82(3), 1998, pp. 147-160

Abstract

The occupancy of the atypical neuroleptic quetiapine (Seroquel) at the D-2 dopamine receptor was investigated using the PET tracers [C-11]raclopride and N-[C-11]methylspiperone in a group of five schizophrenicpatients. A steady-state treatment condition was ensured by dosing the patients with 750 mg quetiapine daily during 3 weeks followed by a period of tapering off the dose. For each patient, PET examinations were performed with both tracers at two of the following doses: 750, 450,300 and/or 150 mg. As control, a group of six healthy untreated volunteers was investigated. The D-2, binding potential in the putamen and the caudate nucleus was determined by using an evaluation method basedon the method proposed by Patlak and Blasberg. The receptor occupancywas determined by assuming that the group of healthy volunteers is representative of untreated drug-naive schizophrenic patients. While a significant linear trend of increasing occupancy with increasing quetiapine dose (reaching 51% +/- 10% occupancy at the 750 mg dose) was detected with [C-11]raclopride (P < 0.01), no such trend was apparent for N-[C-11]methylspiperone (P > 0.09, maximal occupancy values were 2% +/- 3%, measured for the group of three patients on 450 mg). The study suggests that N-[C-11]methylspiperone cannot be used for the assessmentof D-2, receptor occupancy induced by quetiapine. The result is discussed in terms of endogenous dopamine, tracer kinetics and equilibrium dissociation constants. (C) 1998 Elsevier Science Ireland Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/01/20 alle ore 13:56:19