Martinot J L, Paillère-Martinot M L, Poirier M F, Dao-Castellana M H, Loc'h C, Mazière B
Service Hospitalier Frédéric Joliot, CEA and INSERM U334, Orsay, France.
Psychopharmacology (Berl). 1996 Mar;124(1-2):154-8. doi: 10.1007/BF02245616.
The relationship between the daily oral dose of the benzamide amisulpride and the striatal D2-dopamine receptors occupancy was investigated in 11 schizophrenic patients using positron emission tomography with 76Br-bromolisuride. The patients were studied before and during chronic treatment with amisulpride over a wide range of doses. The test-retest variability of the method was estimated to be 5.8% in a group of four patients receiving placebo. A curvilinear relationship was demonstrated between the amisulpride doses and the D2-receptor occupancy. A range of 70-80% occupancy of the striatal D2 receptors, suggested as an optimal interval for therapeutic action on positive psychotic symptoms, was obtained with doses of amisulpride ranging between 630 and 910 mg per day, while an occupancy of 85%, suggested to be associated with pronounced extrapyramidal side-effects, was reached with 1,100 mg per day.
采用正电子发射断层扫描技术及76Br-溴隐亭，对11例精神分裂症患者进行研究，以探讨苯甲酰胺类药物氨磺必利的每日口服剂量与纹状体D2-多巴胺受体占有率之间的关系。在氨磺必利广泛剂量范围内的慢性治疗前后对患者进行研究。在一组接受安慰剂的4名患者中，该方法的重测变异性估计为5.8%。氨磺必利剂量与D2受体占有率之间呈曲线关系。对于阳性精神病性症状的治疗作用，建议最佳区间为纹状体D2受体占有率达到70%-80%，每日氨磺必利剂量在630至910毫克之间时可达到该占有率；而当每日剂量为1100毫克时，占有率达到85%，这被认为与明显的锥体外系副作用相关。
