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[F]AldoView 的研发：首个用于原发性醛固酮增多症成像的高度选择性醛固酮合酶 PET 示踪剂。

Development of [F]AldoView as the First Highly Selective Aldosterone Synthase PET Tracer for Imaging of Primary Hyperaldosteronism.

机构信息

Centre for Radiopharmaceutical Chemistry, University College London, 5 Gower Place, London WC1E 6BS, U.K.

William Harvey Research Institute, Barts & The London School of Medicine & Dentistry, Queen Mary University of London, Charterhouse Square, London EC1M 6BQ, U.K.

出版信息

J Med Chem. 2021 Jul 8;64(13):9321-9329. doi: 10.1021/acs.jmedchem.1c00539. Epub 2021 Jun 17.

DOI:10.1021/acs.jmedchem.1c00539
PMID:34137616
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8273890/
Abstract

The purpose of this study was to synthesize a fluorine-18 labeled, highly selective aldosterone synthase (CYP11B2) inhibitor, [F]AldoView, and to assess its potential for the detection of aldosterone-producing adenomas (APAs) with positron emission tomography in patients with primary hyperaldosteronism (PHA). Using dibenzothiophene sulfonium salt chemistry, [F]AldoView was obtained in high radiochemical yield in one step from [F]fluoride. In mice, the tracer showed a favorable pharmacokinetic profile, including rapid distribution and clearance. Imaging in the adrenal tissue from patients with PHA revealed diffuse binding patterns in the adrenal cortex, avid binding in some adenomas, and "hot spots" consistent with aldosterone-producing cell clusters. The binding pattern was in good visual agreement with the antibody staining of CYP11B2 and distinguished areas with normal and excessive CYP11B2 expression. Taken together, [F]AldoView is a promising tracer for the detection of APAs in patients with PHA.

摘要

本研究旨在合成一种氟-18 标记的、高选择性的醛固酮合酶（CYP11B2）抑制剂[F]AldoView，并评估其在原发性醛固酮增多症（PHA）患者中通过正电子发射断层扫描检测醛固酮分泌腺瘤（APA）的潜力。使用二苯并噻吩𬭩盐化学，[F]AldoView 可从[F]氟化物一步以高放射化学产率获得。在 PHA 患者的肾上腺组织中进行成像显示，在肾上腺皮质中呈现弥漫性结合模式，一些腺瘤中存在强烈结合，以及与醛固酮产生细胞簇一致的“热点”。该结合模式与 CYP11B2 的抗体染色具有良好的视觉一致性，并区分了具有正常和过度 CYP11B2 表达的区域。总之，[F]AldoView 是一种有前途的示踪剂，可用于检测 PHA 患者中的 APA。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/7fe8ff3841e2/jm1c00539_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/7246f9473367/jm1c00539_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/2a76cc930df2/jm1c00539_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/8503d463453a/jm1c00539_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/7fe8ff3841e2/jm1c00539_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/7246f9473367/jm1c00539_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/2a76cc930df2/jm1c00539_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/8503d463453a/jm1c00539_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bef/8273890/7fe8ff3841e2/jm1c00539_0003.jpg

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