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体内评估针对黑色素聚集激素受体 1 的放射性示踪剂：[C]SNAP-7941 和 [F]FE@SNAP 显示在心室系统中有特异性摄取。

In vivo evaluation of radiotracers targeting the melanin-concentrating hormone receptor 1: [C]SNAP-7941 and [F]FE@SNAP reveal specific uptake in the ventricular system.

机构信息

Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Vienna, Austria.

Department of Engineering, University of Applied Sciences Wiener Neustadt, Wiener Neustadt, Austria.

出版信息

Sci Rep. 2017 Aug 14;7(1):8054. doi: 10.1038/s41598-017-08684-6.

DOI:10.1038/s41598-017-08684-6
PMID:28808288
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5556108/
Abstract

The MCHR1 is involved in the regulation of energy homeostasis and changes of the expression are linked to a variety of associated diseases, such as diabetes and adiposity. The study aimed at the in vitro and in vivo evaluation of [C]SNAP-7941 and [F]FE@SNAP as potential PET-tracers for the MCHR1. Competitive binding studies with non-radioactive derivatives and small-animal PET/CT and MRI brain studies were performed under baseline conditions and tracer displacement with the unlabelled MCHR1 antagonist (±)-SNAP-7941. Binding studies evinced high binding affinity of the non-radioactive derivatives. Small-animal imaging of [C]SNAP-7941 and [F]FE@SNAP evinced high tracer uptake in MCHR1-rich regions of the ventricular system. Quantitative analysis depicted a significant tracer reduction after displacement with (±)-SNAP-7941. Due to the high binding affinity of the non-labelled derivatives and the high specific tracer uptake of [C]SNAP-7941 and [F]FE@SNAP, there is strong evidence that both radiotracers may serve as highly suitable agents for specific MCHR1 imaging.

摘要

MCHR1 参与能量稳态的调节，其表达的变化与多种相关疾病有关，如糖尿病和肥胖症。本研究旨在对 [C]SNAP-7941 和 [F]FE@SNAP 进行体外和体内评估，作为 MCHR1 的潜在 PET 示踪剂。使用非放射性衍生物和小动物 PET/CT 和 MRI 脑研究进行竞争性结合研究，并在基线条件下和用未标记的 MCHR1 拮抗剂（±）-SNAP-7941 进行示踪剂置换进行研究。结合研究表明非放射性衍生物具有高结合亲和力。[C]SNAP-7941 和 [F]FE@SNAP 的小动物成像显示在脑室系统中 MCHR1 丰富的区域有高示踪剂摄取。定量分析表明，在用（±）-SNAP-7941 置换后，示踪剂明显减少。由于非标记衍生物的高结合亲和力和 [C]SNAP-7941 和 [F]FE@SNAP 的高特异性示踪剂摄取，有强有力的证据表明这两种放射性示踪剂都可能作为特异性 MCHR1 成像的高度合适的试剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/75a7d49e9b05/41598_2017_8684_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/fab77482a2e9/41598_2017_8684_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/3ea23f107360/41598_2017_8684_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/5deafaafb8a8/41598_2017_8684_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/4f736b3d309f/41598_2017_8684_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/522b0c01261d/41598_2017_8684_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/b7c23ca9ed95/41598_2017_8684_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/75a7d49e9b05/41598_2017_8684_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/fab77482a2e9/41598_2017_8684_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/3ea23f107360/41598_2017_8684_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/5deafaafb8a8/41598_2017_8684_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/4f736b3d309f/41598_2017_8684_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/522b0c01261d/41598_2017_8684_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/b7c23ca9ed95/41598_2017_8684_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04aa/5556108/75a7d49e9b05/41598_2017_8684_Fig7_HTML.jpg

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Bioorg Med Chem. 2012 Oct 1;20(19):5936-40. doi: 10.1016/j.bmc.2012.07.051. Epub 2012 Aug 7.
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