title: Dopamine D2 receptor occupancy in vivo by the novel atypical antipsychotic olanzapine--a 123I IBZM single photon emission tomography (SPET) study.
abstract: We have studied striatal D2 dopamine binding in schizophrenic patients treated with the novel atypical antipsychotic drug, olanzapine. 123I iodobenzamide (IBZM) single photon emission tomography (SPET) was used to estimate striatal dopamine D2 receptor binding in vivo. Patients were recruited from a prospective, double blind controlled trial of olanzapine versus haloperidol treatment. In vivo striatal D2 binding data from olanzapine treated patients (n = 6) were compared with previously reported data from typical antipsychotic responsive (n = 10); clozapine (n = 10); and risperidone (n = 6) treated patient groups. Mean % Brief Psychiatric Rating Scale score (BPRS) improvement following olanzapine treatment was 49% (SD 44). The hypothesis that clinical improvement in olanzapine treated patients would be associated with higher mean striatal D2 binding of 123I IBZM (reflecting lower levels of D2 occupancy) than typical antipsychotic (1.25 +/- 0.05) or risperidone (1.24 +/- 0.04) treatment was confirmed. Olanzapine treated patients had similar levels of striatal D2 binding in vivo (1.41 +/- 0.06) as those treated with clozapine (1.49 +/- 0.04). This preliminary evidence suggests olanzapine is another atypical antipsychotic drug in which therapeutic response is not associated with a high degree of striatal D2 receptor occupancy in vivo.
authors.affiliation: Institute of Psychiatry, London, UK.
authors.forename: L S
authors.initials: LS
authors.lastname: Pilowsky
authors.forename: G F
authors.initials: GF
authors.lastname: Busatto
authors.forename: M
authors.initials: M
authors.lastname: Taylor
authors.forename: D C
authors.initials: DC
authors.lastname: Costa
authors.forename: T
authors.initials: T
authors.lastname: Sharma
authors.forename: T
authors.initials: T
authors.lastname: Sigmundsson
authors.forename: P J
authors.initials: PJ
authors.lastname: Ell
authors.forename: V
authors.initials: V
authors.lastname: Nohria
authors.forename: R W
authors.initials: RW
authors.lastname: Kerwin
mesh_terms: D000328:Adult; D014150:Antipsychotic Agents / Q000378:metabolism*; D001549:Benzamides; D001569:Benzodiazepines; D003342:Corpus Striatum / Q000000981:diagnostic imaging / Q000378:metabolism*; D006220:Haloperidol / Q000378:metabolism; D006801:Humans; D008875:Middle Aged; D000077152:Olanzapine; D010890:Pirenzepine / Q000031:analogs & derivatives* / Q000494:pharmacology; D011759:Pyrrolidines; D017448:Receptors, Dopamine D2 / Q000378:metabolism*; D012559:Schizophrenia / Q000000981:diagnostic imaging / Q000378:metabolism*; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D014150:Antipsychotic Agents; D001549:Benzamides; D011759:Pyrrolidines; D017448:Receptors, Dopamine D2; D001569:Benzodiazepines; D010890:Pirenzepine; C055743:3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide; D006220:Haloperidol; D000077152:Olanzapine