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Extrastriatal dopamine D2 receptor occupancy in olanzapine-treated patients with schizophrenia

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Abstract

Olanzapine is described as a multi-acting receptor-targeted antipsychotic agent. Although regional differences of dopamine D2 receptor occupancy, i.e., limbic selectivity, were reported for olanzapine, contradictory results were also reported. We measured dopamine D2 receptor occupancy of olanzapine in extrastriatal regions in patients with schizophrenia using positron-emission tomography with [11C]FLB457 and the plasma concentrations of olanzapine. Ten patients with schizophrenia taking 5–20 mg/day of olanzapine participated. Dopamine D2 receptor occupancy in the temporal cortex ranged from 61.1 to 85.8%, and plasma concentration was from 12.7 to 115.4 ng/ml. The ED50 value was 3.4 mg/day for dose and 10.5 ng/ml for plasma concentration. The ED50 values obtained in this study were quite similar to those previously reported in the striatum. In conclusion, although the subjects and methods were different from previous striatal occupancy studies, these results suggest that limbic occupancy by olanzapine may not be so different from that in the striatum.

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Acknowledgments

This study was supported by a consignment expense for the Molecular Imaging Program on “Research Base for PET Diagnosis” from the Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japanese Government. We thank Mr. Katsuyuki Tanimoto, Mr. Takahiro Shiraishi, Mr. Akira Ando, and Mr. Toshio Miyamoto for their assistance in performing the PET experiments, and Ms. Yoshiko Fukushima for her help as clinical research coordinator at the National Institute of Radiological Sciences. We thank also Dr. Amane Tateno, Dr. Mizuho Sekine, and Dr. Hajime Fukuta for their clinical support.

Conflict of interest statement

All authors reported no conflict of interest.

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Authors and Affiliations

  1. Molecular Neuroimaging Group, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1, Anagawa, Inage-ku, Chiba, 263-8555, Japan

    Ryosuke Arakawa, Hiroshi Ito, Masaki Okumura, Akihiro Takano, Hidehiko Takahashi, Harumasa Takano & Tetsuya Suhara

  2. Department of Neuropsychiatry, Nippon Medical School, 1-1-5, Sendagi, Bunkyo-ku, Tokyo, Japan

    Ryosuke Arakawa, Masaki Okumura & Yoshiro Okubo

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  1. Ryosuke Arakawa
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Correspondence to Tetsuya Suhara.

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Arakawa, R., Ito, H., Okumura, M. et al. Extrastriatal dopamine D2 receptor occupancy in olanzapine-treated patients with schizophrenia. Eur Arch Psychiatry Clin Neurosci 260, 345–350 (2010). https://doi.org/10.1007/s00406-009-0082-5

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  • DOI: https://doi.org/10.1007/s00406-009-0082-5

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