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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
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- 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.
ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/01/20 alle ore 02:23:00