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Discovery of 6-(Fluoro-18F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([18F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs)
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2016-05-05 00:00:00 , DOI: 10.1021/acs.jmedchem.6b00166 Abbas M. Walji 1 , Eric D. Hostetler 2 , Harold Selnick 1 , Zhizhen Zeng 2 , Patricia Miller 2 , Idriss Bennacef 2 , Cristian Salinas 2 , Brett Connolly 2 , Liza Gantert 2 , Marie Holahan 2 , Stacey O’Malley 2 , Mona Purcell 2 , Kerry Riffel 2 , Jing Li 3 , Jaume Balsells 3 , Julie A. OBrien 4 , Stacey Melquist 4 , Aileen Soriano 5 , Xiaoping Zhang 5 , Aimie Ogawa 5 , Serena Xu 5 , Elizabeth Joshi 6 , Joseph Della Rocca 7 , Fred J. Hess 8 , Joel Schachter 8 , David Hesk 9 , David Schenk 9 , Arie Struyk 10 , Kerim Babaoglu 11 , Talakad G. Lohith 2 , Yaode Wang 12 , Kun Yang 12 , Jianmin Fu 12 , Jeffrey L. Evelhoch 2 , Paul J. Coleman 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2016-05-05 00:00:00 , DOI: 10.1021/acs.jmedchem.6b00166 Abbas M. Walji 1 , Eric D. Hostetler 2 , Harold Selnick 1 , Zhizhen Zeng 2 , Patricia Miller 2 , Idriss Bennacef 2 , Cristian Salinas 2 , Brett Connolly 2 , Liza Gantert 2 , Marie Holahan 2 , Stacey O’Malley 2 , Mona Purcell 2 , Kerry Riffel 2 , Jing Li 3 , Jaume Balsells 3 , Julie A. OBrien 4 , Stacey Melquist 4 , Aileen Soriano 5 , Xiaoping Zhang 5 , Aimie Ogawa 5 , Serena Xu 5 , Elizabeth Joshi 6 , Joseph Della Rocca 7 , Fred J. Hess 8 , Joel Schachter 8 , David Hesk 9 , David Schenk 9 , Arie Struyk 10 , Kerim Babaoglu 11 , Talakad G. Lohith 2 , Yaode Wang 12 , Kun Yang 12 , Jianmin Fu 12 , Jeffrey L. Evelhoch 2 , Paul J. Coleman 1
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Neurofibrillary tangles (NFTs) made up of aggregated tau protein have been identified as the pathologic hallmark of several neurodegenerative diseases including Alzheimer’s disease. In vivo detection of NFTs using PET imaging represents a unique opportunity to develop a pharmacodynamic tool to accelerate the discovery of new disease modifying therapeutics targeting tau pathology. Herein, we present the discovery of 6-(fluoro-18F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine, 6 ([18F]-MK-6240), as a novel PET tracer for detecting NFTs. 6 exhibits high specificity and selectivity for binding to NFTs, with suitable physicochemical properties and in vivo pharmacokinetics.
中文翻译：
发现6-（氟18 F）-3-（1 H-吡咯并[2,3- c ]吡啶-1-基）异喹啉-5-胺（[ 18 F] -MK-6240）：正电子发射定量成像（PET）成像剂，用于定量神经原纤维缠结（NFT）
由聚集的tau蛋白组成的神经原纤维缠结（NFTs）已被确定为包括阿尔茨海默氏病在内的几种神经退行性疾病的病理学标志。使用PET成像对NFT进行体内检测代表了开发药效学工具以加速发现针对tau病理学的新疾病修饰疗法的独特机会。在这里，我们介绍了6-（氟-18 F）-3-（1 H-吡咯并[2,3- c ]吡啶-1-基）异喹啉-5-胺，6（[ 18 F] -MK -6240），作为检测NFT的新型PET示踪剂。6 具有与NFTs结合的高特异性和选择性，具有合适的理化性质和体内药代动力学。
更新日期：2016-05-05
中文翻译：
发现6-（氟18 F）-3-（1 H-吡咯并[2,3- c ]吡啶-1-基）异喹啉-5-胺（[ 18 F] -MK-6240）：正电子发射定量成像（PET）成像剂，用于定量神经原纤维缠结（NFT）
由聚集的tau蛋白组成的神经原纤维缠结（NFTs）已被确定为包括阿尔茨海默氏病在内的几种神经退行性疾病的病理学标志。使用PET成像对NFT进行体内检测代表了开发药效学工具以加速发现针对tau病理学的新疾病修饰疗法的独特机会。在这里，我们介绍了6-（氟-18 F）-3-（1 H-吡咯并[2,3- c ]吡啶-1-基）异喹啉-5-胺，6（[ 18 F] -MK -6240），作为检测NFT的新型PET示踪剂。6 具有与NFTs结合的高特异性和选择性，具有合适的理化性质和体内药代动力学。
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