Molecular Imaging Center, National Institute of Radiological Sciences, Inage-ku, Chiba, 263-8555, Japan.
Eur Arch Psychiatry Clin Neurosci. 2010 Jun;260(4):345-50. doi: 10.1007/s00406-009-0082-5. Epub 2009 Oct 23.
Olanzapine is described as a multi-acting receptor-targeted antipsychotic agent. Although regional differences of dopamine D(2) receptor occupancy, i.e., limbic selectivity, were reported for olanzapine, contradictory results were also reported. We measured dopamine D(2) receptor occupancy of olanzapine in extrastriatal regions in patients with schizophrenia using positron-emission tomography with [(11)C]FLB457 and the plasma concentrations of olanzapine. Ten patients with schizophrenia taking 5-20 mg/day of olanzapine participated. Dopamine D(2) 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 ED(50) value was 3.4 mg/day for dose and 10.5 ng/ml for plasma concentration. The ED(50) 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.
奥氮平被描述为一种多作用受体靶向抗精神病药物。尽管有报道称奥氮平在不同区域对多巴胺 D2 受体的占有率存在差异，即边缘选择性，但也有相反的结果报道。我们使用 [(11)C]FLB457 正电子发射断层扫描和奥氮平的血浆浓度，测量了精神分裂症患者的外纹状体区域奥氮平的多巴胺 D2 受体占有率。10 名服用 5-20 毫克/天奥氮平的精神分裂症患者参与了这项研究。颞叶皮层的多巴胺 D2 受体占有率范围为 61.1%至 85.8%，血浆浓度范围为 12.7 至 115.4ng/ml。剂量的 ED50 值为 3.4 毫克/天，血浆浓度的 ED50 值为 10.5ng/ml。本研究中获得的 ED50 值与以前在纹状体中报道的值非常相似。总之，尽管研究对象和方法与以前的纹状体占有率研究不同，但这些结果表明，奥氮平对边缘系统的占有率可能与纹状体没有太大区别。
