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Bailey, Justin J.; Kaiser, Lena; Lindner, Simon; Wuest, Melinda; Thiel, Alexander; Soucy, Jean-Paul; Rosa-Neto, Pedro; Scott, Peter J. H.; Unterrainer, Marcus; Kaplan, David R.; Waengler, Carmen; Waengler, Björn; Bartenstein, Peter; Bernard-Gauthier, Vadim; Schirrmachert, Ralf (2019): First-in-Human Brain Imaging of [F-18]TRACK, a PET tracer for Tropomyosin Receptor Kinases. In: ACS Chemical Neuroscience, Vol. 10, No. 6: pp. 2697-2702
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The tropomyosin receptor kinase TrkA/B/C family is responsible for human neuronal growth, survival, and differentiation from early nervous system development stages onward. Downregulation of TrkA/B/C receptors characterizes numerous neurological disorders including Alzheimer's disease (AD). Abnormally expressed Trk receptors or chimeric Trk fusion proteins are also well-characterized oncogenic drivers in a variety of neurogenic and non-neurogenic human neoplasms and are currently the focus of intensive clinical research. Previously, we have described the clinical translation of a highly selective and potent carbon-11-labeled pan-Trk radioligand and the preclinical characterization of the optimized fluorine-18-labeled analogue, [F-18]TRACK, for in vivo Trk positron emission tomography (PET) imaging. We describe herein central nervous system selectivity assessment and first-in-human study of [F-18]TRACK.