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首页> 美国政府科技报告 >Use of Sup 76 Br-Bromospiperone for the Analysis of Dopamine Receptors in Neuroleptic Treated Patients
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Use of Sup 76 Br-Bromospiperone for the Analysis of Dopamine Receptors in Neuroleptic Treated Patients

机译：使用sup 76 Br-Brom Brosposponeone分析神经炎治疗患者的多巴胺受体

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The determination of the optimal prescription dosage of neuroleptic medications is of great importance to optimize the therapeutic response and to minimize the occurrence of tardive dyskinesia and other side-effects. PET, a non-invasive methodology which provides in-vivo the actual binding (occupation) of brain dopamine receptors, can be used as an in-vivo radioreceptor assay to indirectly estimate the neuroleptic tissue levels. In this study, 76Br-BSP was used in conjunction with PET to provide a semi-quantitative estimate of the neuroleptic (D2) binding sites occupancy rate during and following oral treatment by neuroleptics. On neuroleptic treatment, the fraction of unoccupied sites showed a striking dose-dependence ranging from .94 to .27 for lowest and highest doses. The CPZ equivalent daily oral doses occupying 50 and 100% of the neuroleptic sites were found to be respectively about 6 and 60 mu mol/kg. The results establish that washout of neuroleptics from striatal binding sites is a rapid process that strongly suggest that the long-lasting remissions of psychotic patients following neuroleptic withdrawal are not due to persistent dopamine receptor occupation. (ERA citation 13:016277)

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