In vivo kinetics of [F-18]MEFWAY: a comparison with [C-11]WAY100635 and [F-18]MPPF in the nonhuman primate.
In vivo kinetics of [F-18]MEFWAY: a comparison with [C-11]WAY100635 and [F-18]MPPF in the nonhuman primate.
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DOI：
10.1002/syn.20878
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发表时间：
2011-07
期刊：
影响因子：
2.3
通讯作者：
Christian, B. T.
中科院分区：
文献类型：
--
作者：
Wooten, D. W.;Moraino, J. D.;Hillmer, A. T.;Engle, J. W.;Dejesus, O. J.;Murali, D.;Barnhart, T. E.;Nickles, R. J.;Davidson, R. J.;Schneider, M. L.;Mukherjee, J.;Christian, B. T.
[F-18]Mefway是为了提供一种与5-HT1A受体具有高亲和力的F-18标记的PET神经配体，以改进5-HT1A系统的体内评估。这项工作的目的是比较[F-18]Mefway、[F-18]MPPF和[C-11]WAY100635在恒河猴体内的动力学。四只猴子每人注射[F-18]Mefway、[C-11]WAY100635和[F-18]MPPF，并用microPET P4扫描仪进行扫描。在PET实验的整个时间过程中，采集动脉血以测定母体化合物。在前扣带回皮质(ACG)、内侧颞叶皮质(MTC)、中缝核(RN)和岛叶皮质(IC)的5-HT1a高结合区提取时间活动曲线。以小脑(CB)为参照区，提取时间活动曲线。根据非置换分布体积(VND)和结合电势(BPND)比较了放射性示踪剂的体内动力学。在30min时，母体化合物在血浆中的放射性分数分别为19%、28%和29%，并以0.0031、0.0078和0.0069(分钟-1)的速率从动脉血浆中清除(中途，[F-18]MPPF，[C-11]WAY100635)。脑区BPND分别为：MTC：7.4±0.6，3.1±0.4，7.0±1.2，ACG：7.2±1.2，2.1±0.2，7.9±1.2；RN：3.7±0.6，1.3±0.3，3.3±0.7；IC：4.2±0.6，1.2±0.1，4.7±1.0。在恒河猴体内，[F-18]Mefway的体内动力学与[C-11]WAY100635相似，BPND的产量比[F-18]MPPF高2倍以上。这些特性使[F-18]成为5-HT1A分析的一种有希望的放射性示踪剂，在BPND中提供了更高的计数统计和更大的动态范围。
[F-18]Mefway was developed to provide an F-18 labeled PET neuroligand with high affinity for the serotonin 5-HT1A receptor to improve the in vivo assessment of the 5-HT1A system. The goal of this work was to compare the in vivo kinetics of [F-18]mefway, [F-18]MPPF, and [C-11]WAY100635 in the rhesus monkey. Each of four monkeys were given bolus injections of [F-18]mefway, [C-11]WAY100635, and [F-18]MPPF and scans were acquired with a microPET P4 scanner. Arterial blood was sampled to assay parent compound throughout the time course of the PET experiment. Time activity curves were extracted in the high 5-HT1A binding areas of the anterior cingulate cortex (ACG), mesial temporal cortex (MTC), raphe nuclei (RN) and insula cortex (IC). Time activity curves were also extracted in the cerebellum (CB) which was used as a reference region. The in vivo kinetics of the radiotracers were compared based upon the nondisplaceable distribution volume (VND) and binding potential (BPND). At 30 minutes, the fraction of radioactivity in the plasma due to parent compound was 19%, 28%, and 29% and cleared from the arterial plasma at rates of 0.0031, 0.0078, and 0.0069 (min-1) ([F-18]mefway, [F-18]MPPF, [C-11]WAY100635). The BPND in the brain regions were; MTC: 7.4±0.6, 3.1±0.4, 7.0±1.2, ACG: 7.2±1.2, 2.1±0.2, 7.9±1.2; RN: 3.7±0.6, 1.3±0.3, 3.3±0.7 and IC: 4.2±0.6, 1.2±0.1, 4.7±1.0 for [F-18]mefway, [F-18]MPPF, and [C-11]WAY100635 respectively. In the rhesus monkey, [F-18]mefway has similar in vivo kinetics to [C-11]WAY100635 and yields greater than 2-fold higher BPND than [F-18]MPPF. These properties make [F-18]mefway a promising radiotracer for 5-HT1A assay, providing higher counting statistics and a greater dynamic range in BPND.
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影响因子：
4.6
作者：
DELFORGE, J;SYROTA, A;MAZOYER, BM
通讯作者：
MAZOYER, BM
影响因子：
6.3
作者：
KOEPPE, RA;FREY, KA;KUHL, DE
通讯作者：
KUHL, DE
影响因子：
6.3
作者：
Parsey, RV;Arango, V;Mann, JJ
通讯作者：
Mann, JJ
DOI：
10.1007/s002590050211
发表时间：
1998-02-01
期刊：
EUROPEAN JOURNAL OF NUCLEAR MEDICINE
影响因子：
--
作者：
Hume, SP;Gunn, RN;Jones, T
通讯作者：
Jones, T
影响因子：
6.8
作者：
AKAIKE, H
通讯作者：
AKAIKE, H