Article
Clinical Neurology
Eric E. Abrahamson, Julia K. Kofler, Carl R. Becker, Julie C. Price, Kathy L. Newell, Bernardino Ghetti, Jill R. Murrell, Catriona A. McLean, Oscar L. Lopez, Chester A. Mathis, William E. Klunk, Victor L. Villemagne, Milos D. Ikonomovic
Summary: In a post-mortem study, it has been found that the amyloid PET radioligand Pittsburgh compound B (PiB) interacts poorly with cotton wool plaques, which are common in familial Alzheimer's disease but rare in sporadic Alzheimer's disease. This limited interaction may lead to an underestimation of total amyloid burden in patients with familial Alzheimer's disease.
Article
Clinical Neurology
William Charles Kreisl, Patrick J. Lao, Aubrey Johnson, Zeljko Tomljanovic, Julia Klein, Krista Polly, Benjamin Maas, Krystal K. Laing, Anthony G. Chesebro, Kay Igwe, Qolamreza R. Razlighi, Lawrence S. Honig, Xinyu Yan, Seonjoo Lee, Akiva Mintz, Jose A. Luchsinger, Yaakov Stern, D. P. Devanand, Adam M. Brickman
Summary: F-18-MK-6240 showed good correlation with CSF tau and p-tau levels, as well as age, cognition, and amyloid-based AD biomarkers. The study also found that F-18-MK-6240 binding patterns were associated with specific cognitive impairments in amyloid-positive participants, reflecting the progression of AD pathology.
ALZHEIMERS & DEMENTIA
(2022)
Article
Biochemistry & Molecular Biology
Wei Zheng, Yong Huang, Hualong Chen, Zeng Jiang, Ziyue Yu, Tingyu Yang, Lu Zhang, Xuebo Cheng, Yajing Liu, Qi Liu, Xunming Ji, Zehui Wu
Summary: Accurate quantification of amyloid beta (AO') plaques is crucial for the diagnosis and treatment of Alzheimer's disease. New highly sensitive tracers, such as [18F]BIBD-124, were developed with improved clearance rates and lower in vivo defluorination compared to AV45. These tracers showed similar binding sites and imaging capabilities to AV45, with better imaging contrast and less nonspecific uptake. Based on these promising results, [18F]BIBD-124 is expected to be a potential radiotracer for further clinical trials.
ACS CHEMICAL NEUROSCIENCE
(2023)
Review
Pharmacology & Pharmacy
Chao Wang, Rong Lin, Shaobo Yao
Summary: This review focuses on recent advances in the synthesis, radiolabeling, and application of a series of F-18-labeled amino acid analogs using new F-18-labeling strategies.
Article
Chemistry, Organic
Min Ho Jeon, Young-Do Kwon, Min Pyeong Kim, Gianluca Bartolini Torres, Jeong Kon Seo, Jeongmin Son, Young Hoon Ryu, Sung You Hong, Joong-Hyun Chun
Summary: The study presents a successful synthesis of various sulfamoyl [F-18]fluorides using an F-18/F-19 isotopic exchange approach, improving synthetic efficiency with radiochemical yields up to 97%. This late-stage labeling protocol offers an efficient route to diversify the chemical library possessing sulfamoyl functionalities by incorporating nucleophilic F-18 within nitrogen-containing sulfur(VI) frameworks.
Article
Medicine, General & Internal
Cecile Tissot, Joseph Therriault, Peter Kunach, Andrea L. Benedet, Tharick A. Pascoal, Nicholas J. Ashton, Thomas K. Karikari, Stijn Servaes, Firoza Z. Lussier, Mira Chamoun, Dana L. Tudorascu, Jenna Stevenson, Nesrine Rahmouni, Nina Margherita Poltronetti, Vanessa Pallen, Gleb Bezgin, Min Su Kang, Sulantha S. Mathotaarachchi, Yi-Ting Wang, Jaime Fernandez Arias, Pamela Cristina Lukasewicz Ferreira, Joao Pedro Ferrari-Souza, Eugeen Vanmechelen, Kaj Blennow, Henrik Zetterberg, Serge Gauthier, Pedro Rosa-Neto
Summary: This study investigated the agreement between [F-18]MK6240 tau-PET, plasma pTau181, and pTau231 in Alzheimer's disease. The findings suggest that these biomarkers reflect different stages of tau progression and can be useful in diagnosing and evaluating the disease stage.
Article
Medicine, Research & Experimental
Hualong Chen, Zeng Jiang, Xuebo Cheng, Wei Zheng, Yuli Sun, Ziyue Yu, Tingyu Yang, Lu Zhang, Jun Yan, Yajing Liu, Xunming Ji, Zehui Wu
Summary: The short half-life of C-11 limits its clinical application. To overcome this issue, the researchers designed four fluorine-labeled derivatives of ER176 and confirmed their high affinity and suitability in vitro and in vivo. [F-18]BIBD-239 was chosen as a candidate compound for further evaluation due to its simple synthesis conditions and high brain penetration.
MOLECULAR PHARMACEUTICS
(2022)
Article
Radiology, Nuclear Medicine & Medical Imaging
MiaoMiao Xu, Jun Guo, JiaCheng Gu, LinLin Zhang, ZiHao Liu, Lin Ding, HongLiang Fu, YuFei Ma, Sheng Liang, Hui Wang
Summary: A new Aβ tracer [F-18]DRKXH1 was synthesized and evaluated for its performance in diagnosing AD using various methods. The tracer showed promising results in detecting Aβ plaques in the brains of AD transgenic mice and AD patients, suggesting its potential for in vivo detection of the human brain.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Article
Geriatrics & Gerontology
Liping Fu, Jinming Zhang, Kaixiang Zhou, Xiaojun Zhang, Hengge Xie, Mingwei Zhu, Mengchao Cui, Ruimin Wang
Summary: This study evaluates the effectiveness of a new tracer, [F-18]-S16, in distinguishing patients with AD from HCs. The results show that [F-18]-S16 exhibits increased cortical uptake in AD patients, suggesting its potential for in vivo detection of tau protein.
FRONTIERS IN AGING NEUROSCIENCE
(2022)
Article
Biochemistry & Molecular Biology
Thu Hang Lai, Susann Schroeder, Magali Toussaint, Sladjana Dukic-Stefanovic, Mathias Kranz, Friedrich-Alexander Ludwig, Steffen Fischer, Joerg Steinbach, Winnie Deuther-Conrad, Peter Brust, Rares-Petru Moldovan
Summary: This study demonstrated the metabolic stability and specific binding of two fluorinated analogs as PET tracers in the brains of mice, with in vivo PET/MRI studies in CD-1 mice showing high initial brain uptake and rapid clearance for both radiotracers.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Chris Hoffmann, Niklas Kolks, Daniel Smets, Alexander Haseloer, Benedikt Groener, Elizaveta A. Urusova, Heike Endepols, Felix Neumaier, Uwe Ruschewitz, Axel Klein, Bernd Neumaier, Boris D. Zlatopolskiy
Summary: In this study, a series of complexes were systematically evaluated and several generally applicable mediators were identified for highly efficient radiofluorination. The utilization of these mediators significantly improved the labeling yields, even with lower precursor amounts. The practicality of the novel mediators was demonstrated by the efficient production of five PET tracers and transfer of the method to an automated radiosynthesis module.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Medicine, Research & Experimental
Wei Zheng, Xuebo Cheng, Hualong Chen, Zeng Jiang, Yuli Sun, Ziyue Yu, Tingyu Yang, Lu Zhang, Yajing Liu, Xunming Ji, Zehui Wu
Summary: The abnormal expression of aromatase is associated with various neurological diseases and tumors. In this study, F-18 and Ga-68 labeled compounds were designed and synthesized to bind to aromatase. Two of these compounds, BIBD-069 and BIBD-071, showed high affinity for aromatase. They were successfully radiolabeled and specifically bound to aromatase in vitro and in vivo. These compounds can serve as important tools for the diagnosis and treatment of aromatase-related diseases.
MOLECULAR PHARMACEUTICS
(2022)
Article
Chemistry, Medicinal
E. Johanna L. Steen, A. Yeong Park, Wissam Beaino, Changdev Gorakshnath Gadhe, Esther Kooijman, Robert C. Schuit, Maxime Schreurs, Prisca Leferink, Jeroen J. M. Hoozemans, Jae Eun Kim, Jinhwa Lee, Albert D. Windhorst
Summary: This paper reports the development of a positron emission tomography (PET) tracer for potential therapeutic strategy against Parkinson's disease (PD). The tracer shows promising neuroprotective effects and can be used to target c-Abl, a harmful enzyme involved in PD.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Clinical Neurology
Kyoungwon Baik, Seun Jeon, Mincheol Park, Young-gun Lee, Phil Hyu Lee, Young H. Sohn, Byoung Seok Ye
Summary: This study compared the imaging characteristics and cutoff value of 18F-florapronol (FC119S) and 18F-florbetaben (FBB) positron emission tomography (PET) in detecting 3-amyloid positivity and Alzheimer's disease (AD) in patients with cognitive impairment. The findings showed that quantitative FC119S-PET analysis provided reliable information for detecting 3-amyloid deposition and the presence of AD.
JOURNAL OF CLINICAL NEUROLOGY
(2023)
Article
Chemistry, Medicinal
Ayoung Pyo, Misun Yun, Boreum Song, Seong-Young Kwon, Jung-Joon Min, Dong-Yeon Kim
Summary: In this study, 18F-labeled procainamide (PCA) was synthesized and evaluated for its potential as a PET imaging agent for melanoma detection. The results showed that 18F-PCA exhibited high melanoma uptake and could be a promising tool for direct melanoma detection using PET imaging.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)