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Muscarinic receptor occupancy by biperiden in living human brain.

机译:Biperiden在活人脑中占有毒蕈碱受体。

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摘要

Anticholinergic drug is often used to treat extrapyramidal symptoms. We measured muscarinic cholinergic receptor (mAchR) occupancy by the oral administration of biperiden in eight healthy subjects using positron emission tomography (PET) and [11C]N-methyl-4-piperidylbenzilate (NMPB). After the baseline scan each subject underwent one or two post-dose PET scans. mAchR occupancy was 10-45% in the frontal cortex three hours after the oral administration of 4 mg of biperiden. The occupancy correlated with the plasma concentration of biperiden in a curvilinear manner.
机译:抗胆碱能药物通常用于治疗锥体束外症状。我们通过使用正电子发射断层显像(PET)和[11C] N-甲基-4-哌啶基苯甲酸酯(NMPB)在8位健康受试者中口服比哌立定来测量毒蕈碱胆碱能受体(mAchR)的占用。基线扫描后,每个受试者进行一或两次剂量后的PET扫描。口服4 mg的Biperiden后三小时,额叶皮层中的mAchR占用率为10-45%。占有率以曲线方式与比哌立定的血浆浓度相关。

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