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首页> 外文期刊>Journal of Cerebral Blood Flow and Metabolism: Official Journal of the International Society of Cerebral Blood Flow and Metabolism >Quantification of 5-HT2A receptors in the human brain using (18F)altanserin-PET and the bolus/infusion approach.
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Quantification of 5-HT2A receptors in the human brain using (18F)altanserin-PET and the bolus/infusion approach.

机译：使用（18F）altanserin-PET和推注/输注方法对人脑中5-HT2A受体进行定量。

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The aim of the present study is to describe and validate a method for accurate quantification of 5-hydroxytryptamine (5-HT)(2A) receptors using [18F]altanserin-positron emission tomography (PET) and the bolus/infusion approach. A bolus/infusion ratio of 1.75 h aimed at attaining rapid steady state in blood and brain was predicted from previous bolus studies performed in our laboratory. The infusion schedule was tested in normal subjects (n = 10) using dynamic PET and frequent plasma sampling for 6 h. Steady state was attained in brain and plasma within 2 h, and time-activity curves remained constant for another 3 h. To represent free and nonspecifically bound [18F]altanserin and its radiolabeled metabolites only, cerebellum must show no displacement in 5-HT(2A) displacement studies. To validate this, saturating doses of cold ketanserin were administered and it was found that specific binding of [18F]altanserin decreased uniformly to the level of the cerebellum and no change in the cerebellar time-activity curve was found after ketanserin administration. A shorter experimental setup was tested in a second group (n = 20) including patients with neuropsychiatric disorders. Dynamic PET (five frames of 8 minutes each) and venous blood sampling at midscan time started 2 h after [18F]altanserin administration. The mean percentage rate of change per hour in the outcome parameter, DV(3)', was low (mean -0.3% h-1; range -7.3-7.2% h-1) and no correlation of DV(3)' versus time was demonstrated. It is concluded that 5-HT(2A) receptor studies can be conducted within 2 h of [18F]altanserin infusion, yielding reliable results.
机译：本研究的目的是描述和验证一种使用[18F] altanserin-正电子发射断层扫描（PET）和推注/输注方法准确定量5-羟色胺（5-HT）（2A）受体的方法。根据我们实验室先前进行的推注研究，预计将达到1.75 h的推注/输注比，旨在达到血液和大脑的快速稳定状态。在正常受试者（n = 10）中使用动态PET和频繁的血浆采样6小时对输注时间表进行了测试。 2小时内大脑和血浆达到稳态，时间活动曲线又保持3小时不变。为了仅代表自由和非特异性结合的[18F] altanserin及其放射性标记的代谢物，小脑在5-HT（2A）置换研究中必须没有置换。为了证实这一点，给予了饱和剂量的冷酮色林，发现[18F] altanserin的特异性结合均匀地降低到小脑水平，并且在酮色林给药后未发现小脑时间活动曲线的变化。在第二组（n = 20）中测试了较短的实验设置，其中包括神经精神疾病患者。 [18F] altanserin给药后2小时，开始动态PET（5帧，每帧8分钟）和中扫描时静脉血采样。结果参数DV（3）'的每小时平均变化百分比较低（平均值-0.3％h-1;范围-7.3-7.2％h-1），并且DV（3）'与时间被证明了。结论是，可以在[18F] altanserin输注后2小时内进行5-HT（2A）受体研究，得出可靠的结果。

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