CENTRAL D2-DOPAMINE RECEPTOR OCCUPANCY IN RELATION TO ANTIPSYCHOTIC DRUG EFFECTS - A DOUBLE-BLIND PET STUDY OF SCHIZOPHRENIC-PATIENTS
CENTRAL D2-DOPAMINE RECEPTOR OCCUPANCY IN RELATION TO ANTIPSYCHOTIC DRUG EFFECTS - A DOUBLE-BLIND PET STUDY OF SCHIZOPHRENIC-PATIENTS
复制标题
DOI：
10.1016/0006-3223(93)90288-o
复制
发表时间：
1993-02-15
影响因子：
10.6
通讯作者：
UPPFELDT, G
中科院分区：
文献类型：
--
作者：
NORDSTROM, AL;FARDE, L;UPPFELDT, G
一项双盲研究检查了中枢 D2-多巴胺受体占用与抗精神病药物作用之间的关系。雷氯必利是用于诱导 D2-多巴胺受体选择性占据的化合物。此外，C-11 标记的雷氯必利是用于通过正电子发射断层扫描 (PET) 测量占用率的放射性配体。 17 名精神分裂症患者被随机分配到三个平行组之一，接受 4 周的每日剂量雷氯必利治疗。 D2 受体占用率是通过 PET 在完成研究的 13 名患者的稳态条件下测定的。抗精神病作用与 D2 受体占用程度之间存在统计学上显着的关系 (p < 0.05)。有锥体外系副作用的患者的 D2 受体占用率显着高于没有锥体外系副作用的患者 (p = 0.02)。 D2-多巴胺受体的选择性占据与精神分裂症患者临床效果之间关系的发现主要为抗精神病药物作用的多巴胺假说提供了新的支持。
The relationship between central D2-dopamine receptor occupancy and antipsychotic drug effects was examined in a double-blind study. Raclopride was the compound used to induce a selective occupancy of the D2-dopamine receptors. In addition, C-11-labeled raclopride was the radioligand used to measure occupancy by positron emission tomography (PET). Seventeen schizophrenic patients were randomly assigned to one of three parallel groups treated for 4 weeks with daily doses of 2, 6, or 12 mg of raclopride. D2-receptor occupancy was determined by PET at steady-state conditions in 13 patients who completed the study. A statistically significant relationship was demonstrated between antipsychotic effect and degree of D2-receptor occupancy (p < 0.05). Patients with extrapyramidal side effects had significantly higher D2-receptor occupancy than those without (p = 0.02). The finding of a relationship between selective occupancy of the D2-dopamine receptors and clinical effects in schizophrenic patients principally provides new support for the dopamine hypothesis of antipsychotic drug action.