Department of Neuropsychiatry, Nippon Medical School, 1-1-5 Sendagi, Bunkyo-ku, Tokyo, 113-8602, Japan.
Psychopharmacology (Berl). 2021 May;238(5):1343-1350. doi: 10.1007/s00213-020-05698-3. Epub 2020 Nov 12.
Unlike other antipsychotics, our previous positron emission tomography (PET) study demonstrated that a single dose of blonanserin occupied dopamine D as well as dopamine D receptors in healthy subjects. However, there has been no study concerning the continued use of blonanserin.
We examined D and D receptor occupancies in patients with schizophrenia who had been treated with blonanserin.
Thirteen patients with schizophrenia participated. PET examinations were performed on patients treated with clinical dosage of blonanserin or olanzapine alone. A crossover design was used in which seven patients switched drugs after the first scan, and PET examinations were conducted again. D and D receptor occupancies were evaluated by [C]-(+)-PHNO. We used nondisplaceable binding potential (BP) of 6 healthy subjects which we previously reported as baseline. To consider the effect of upregulation of D receptor by continued use of antipsychotics, D receptor occupancy by blonanserin in seven subjects who completed 2 PET scans were re-analyzed by using BP of olanzapine condition as baseline.
Average occupancy by olanzapine (10.8 ± 6.0 mg/day) was as follows: caudate 32.8 ± 18.3%, putamen 26.3 ± 18.2%, globus pallidus - 33.7 ± 34.9%, substantia nigra - 112.8 ± 90.7%. Average occupancy by blonanserin (12.8 ± 5.6 mg/day) was as follows: caudate 61.0 ± 8.3%, putamen 55.5 ± 9.5%, globus pallidus 48.9 ± 12.4%, substantia nigra 34.0 ± 20.6%. EC was 0.30 ng/mL for D receptor for caudate and putamen (df = 19, p < 0.0001) and 0.70 ng/mL for D receptor for globus pallidus and substantia nigra (df = 19, p < 0.0001). EC for D receptor of blonanserin changed to 0.22 ng/mL (df = 13, p = 0.0041) when we used BP of olanzapine condition as baseline.
Our study confirmed that blonanserin occupied both D and D receptors in patients with schizophrenia.
与其他抗精神病药不同，我们之前的正电子发射断层扫描（PET）研究表明，单剂量的布南色林在健康受试者中占据了多巴胺 D 受体和多巴胺 D 受体。然而，尚未有关于布南色林持续使用的研究。
我们检查了接受布南色林治疗的精神分裂症患者的 D 受体和 D 受体占有率。
13 名精神分裂症患者参加了该项研究。对接受布南色林或奥氮平单一治疗的患者进行了 PET 检查。采用交叉设计，7 名患者在第一次扫描后换用药物，再次进行 PET 检查。通过 [C]-(+)-PHNO 评估 D 和 D 受体占有率。我们使用了之前报告的 6 名健康受试者的不可置换结合潜能（BP）作为基线。为了考虑抗精神病药物持续使用对 D 受体上调的影响，我们使用奥氮平条件下的 BP 对完成了 2 次 PET 扫描的 7 名患者的布南色林 D 受体占有率进行了重新分析。
奥氮平（10.8 ± 6.0 mg/天）的平均占有率如下：尾状核 32.8 ± 18.3%，壳核 26.3 ± 18.2%，苍白球 - 33.7 ± 34.9%，黑质 - 112.8 ± 90.7%。布南色林（12.8 ± 5.6 mg/天）的平均占有率如下：尾状核 61.0 ± 8.3%，壳核 55.5 ± 9.5%，苍白球 48.9 ± 12.4%，黑质 34.0 ± 20.6%。尾状核和壳核 D 受体的 EC 为 0.30 ng/mL（df = 19，p < 0.0001），苍白球和黑质 D 受体的 EC 为 0.70 ng/mL（df = 19，p < 0.0001）。当我们使用奥氮平条件下的 BP 作为基线时，布南色林 D 受体的 EC 变为 0.22 ng/mL（df = 13，p = 0.0041）。
我们的研究证实，布南色林在精神分裂症患者中同时占据了 D 受体和 D 受体。
