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Titolo:
In vitro extrastriatal and striatal D-2 dopamine receptor blockade by amisulpride in schizophrenia
Autore:
Xiberas, X; Martinot, JL; Mallet, L; Artiges, E; Canal, M; Loch, C; Maziere, B; Paillere-Martinot, ML;
Indirizzi:
INSERM, U334, Serv Hosp Frederic Joliot, DSV,DRM,CEA, F-91401 Orsay, France INSERM Orsay France F-91401 c Joliot, DSV,DRM,CEA, F-91401 Orsay, France Sanofi Synthelabo, Chilly Mazarin, France Sanofi Synthelabo Chilly Mazarin France thelabo, Chilly Mazarin, France A Chenevier Hosp, Dept Psychiat, Creteil, France A Chenevier Hosp Creteil France er Hosp, Dept Psychiat, Creteil, France Hop La Pitie Salpetriere, APHP, Dept Psychiat, Paris, France Hop La Pitie Salpetriere Paris France PHP, Dept Psychiat, Paris, France
Titolo Testata:
JOURNAL OF CLINICAL PSYCHOPHARMACOLOGY
fascicolo: 2, volume: 21, anno: 2001,
pagine: 207 - 214
SICI:
0271-0749(200104)21:2<207:IVEASD>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
NEGATIVE SYMPTOMS; HUMAN-BRAIN; BINDING; PET; NEUROLEPTICS; OCCUPANCY; SELECTIVITY; AGENTS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
33
Recensione:
Indirizzi per estratti:
Indirizzo: Martinot, JL INSERM, U334, Serv Hosp Frederic Joliot, DSV,DRM,CEA, 4 Pl GlLeclerc, F-91401 Orsay, France INSERM 4 Pl Gl Leclerc Orsay France F-91401 01 Orsay, France
Citazione:
X. Xiberas et al., "In vitro extrastriatal and striatal D-2 dopamine receptor blockade by amisulpride in schizophrenia", J CL PSYCH, 21(2), 2001, pp. 207-214

Abstract

Amisulpride, a substituted benzamide with high affinity for dopamine D-2 and D-3 receptors only, has been reported to have therapeutic effects on both negative and positive schizophrenic symptoms, although at distinct dose ranges (50-300 mg/day vs. 400-1,200 mg/day). The purpose of this study was to investigate the binding of amisulpride to extrastriatal (i.e., thalamus and temporal cortex) and striatal D-2 dopamine receptors with respect to plasma amisulpride determinations. Ten patients with schizophrenia treated with amisulpride over a wide range of doses (25-1,200 mg/day) were studied. Positron emission tomography images were acquired by using Br-76-FLB-457, a highly specific antagonist of the D-2 and D-3 dopamine receptors. Binding indexes (BI) in the regions studied were estimated with reference to values from six healthy subjects. A curvilinear relationship was demonstrated between plasma concentration of amisulpride and the BI in extrastriatal regions. The BI also varied as a function of plasma concentration in striatum. Furthermore, the data provide evidence for different binding profiles: low plasma concentrations (28-92 ng/mL) induced marked extrastriatal binding and low striatal binding, whereas higher plasma concentrations (>153 ng/ mL) induced marked binding both in extrastriatal and striatal regions. Dose-dependent differential binding profiles of amisulpride to D-2 receptors in extrastriatal and striatal regions were demonstrated, and two therapeutic ranges of plasma concentrations for negative and positive schizophrenic symptoms, respectively, are suggested.

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Documento generato il 28/01/20 alle ore 21:08:41