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Titolo:
Striatal and temporal cortical D2/D3 receptor occupancy by olanzapine and sertindole in vivo: a [I-123]epidepride single photon emission tomography (SPET) study
Autore:
Bigliani, V; Mulligan, RS; Acton, PD; Ohlsen, RI; Pike, VW; Ell, PJ; Gacinovic, S; Kerwin, RW; Pilowsky, LS;
Indirizzi:
Inst Psychiat, London SE5 8AF, England Inst Psychiat London England SE5 8AF t Psychiat, London SE5 8AF, England Inst Nucl Med, London W1N 8AA, England Inst Nucl Med London England W1N 8AA t Nucl Med, London W1N 8AA, England Hammersmith Hosp, Imperial Coll, Sch Med, MRC,Cyclotron Unit,Chem & Engn Grp, London W12 ONN, England Hammersmith Hosp London England W12 ONN ngn Grp, London W12 ONN, England
Titolo Testata:
PSYCHOPHARMACOLOGY
fascicolo: 2, volume: 150, anno: 2000,
pagine: 132 - 140
Fonte:
ISI
Lingua:
ENG
Soggetto:
EXTRASTRIATAL D-2-DOPAMINE RECEPTORS; ATYPICAL ANTIPSYCHOTIC OLANZAPINE; CLOZAPINE-TREATED PATIENTS; D-2 DOPAMINE-RECEPTORS; LIVING HUMAN BRAIN; IN-VIVO; SCHIZOPHRENIC-PATIENTS; TYPICAL ANTIPSYCHOTICS; I-125 EPIDEPRIDE; HEALTHY-SUBJECTS;
Keywords:
olanzapine; antipsychotic drug; dopamine D2/D3 receptor; epidepride; single photon emission tomography schizophrenia;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
62
Recensione:
Indirizzi per estratti:
Indirizzo: Pilowsky, LS Inst Psychiat, De Crespigny Pk, Denmark Hill, London SE5 8AF,England Inst Psychiat De Crespigny Pk, Denmark Hill London England SE5 8AF
Citazione:
V. Bigliani et al., "Striatal and temporal cortical D2/D3 receptor occupancy by olanzapine and sertindole in vivo: a [I-123]epidepride single photon emission tomography (SPET) study", PSYCHOPHAR, 150(2), 2000, pp. 132-140

Abstract

Rationale: Previous work suggests clozapine preferentially targets limbic cortical dopamine systems, which could help account for its lack of extrapyramidal side effects (EPS) and superior therapeutic efficacy. Objectives: To test the hypothesis that olanzapine, a novel atypical antipsychotic drug,occupies temporal cortical D3/D3 receptors to a greater extent than striatal D2/D3 receptors in vivo. Methods: Nine schizophrenic patients taking either olanzapine [(n=5: mean (SD) age: 32.5 (6.5) years; daily dose: 18.3 (2.6) mg)] or sertindole [(n=4: mean (SD) age: 30.3 (7.4) years; daily dose: 16 (5.6) mg] were studied with [I-123]epidepride (S)-N-[(1-ethyl- 2-pyrrolidinyl)methyl]-5-iodo-2,3-dimethoxy-benzamide) and single photon emission tomography (SPET). An estimate of [I-123]epidepride 'specific binding' to D2/D3 receptors was obtained in patients and age-matched healthy volunteers. A summary measure was generated representing striatal and temporal cortical relative %D3/D3 receptor occupancy by antipsychotic drugs. Occupancy data were compared with previously studied groups of patients receiving typical antipsychotic drugs (n=12) and clozapine (n=10). Results: Mean striatal and temporal cortical %D2/D3 receptor occupancy in olanzapine-treated patients was 41.3% (SD 17.9) and 82.8% (SD 4.2), respectively. Unexpectedly low levels of striatal relative %D2/D3 receptor occupancy were seen in two patients with typical antipsychotic-drug-induced movement disorder prior to switching to olanzapine. In the temporal cortex, mean D2/D3 dopamine receptor occupancy levels above 80% were seen for all antipsychotic drugs studied. Conclusions: The atypical antipsychotic drugs olanzapine and sertindole, in common with clozapine, demonstrate higher occupancy of temporal cortical than striatal D2/D3 dopamine receptors in vivo at clinically useful doses. This could help mediate their atypical clinical profile of therapeutic efficacy with few extrapyramidal side effects. Limbic selective blockade of D2/D3 dopamine receptors could be a common action of atypical antipsychotic drugs.

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Documento generato il 20/11/19 alle ore 02:32:52