Radiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein
نویسندگان
چکیده
منابع مشابه
Radiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein
Two α-synuclein ligands, 3-methoxy-7-nitro-10H-phenothiazine (2a, Ki = 32.1 ± 1.3 nM) and 3-(2-fluoroethoxy)-7-nitro-10H-phenothiazine (2b, Ki = 49.0 ± 4.9 nM), were radiolabeled as potential PET imaging agents by respectively introducing 11C and 18F. The syntheses of [11C]2a and [18F]2b were accomplished in a good yield with high specific activity. Ex vivo biodistribution studies in rats revea...
متن کاملRadiosynthesis and in Vivo Evaluation of Two PET Radioligands for Imaging α-Synuclein
Two α-synuclein ligands, 3-methoxy-7-nitro-10H-phenothiazine (2a, Ki = 32.1 ± 1.3 nM) and 3-(2-fluoroethoxy)-7-nitro-10H-phenothiazine (2b, Ki = 49.0 ± 4.9 nM), were radiolabeled as potential PET imaging agents by respectively introducing C and F. The syntheses of [C]2a and [F]2b were accomplished in a good yield with high specific activity. Ex vivo biodistribution studies in rats revealed that...
متن کاملSynthesis and in vivo evaluation of novel PET radioligands for imaging the endothelin-A receptor.
UNLABELLED The endothelin subtype-A (ETA) receptor is a member of a family of G-protein-coupled receptors that plays a central role in vasoconstriction, cell proliferation, and hormone production. The aim of this study was to synthesize and evaluate in vivo (11)C- and (18)F-labeled analogs of the potent and selective ETA antagonist N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazol...
متن کاملPET radioligands for in vivo visualization of neuroinflammation.
Neuroinflammation is a well-orchestrated, dynamic, multicellular process playing a major role in neurodegenerative disorders. The microglia which make up the innate immune system of the central nervous system are key cellular mediators of neuroinflammatory processes. In normal condition they exert a protective function, providing tissue repair by releasing anti-inflammatory cytokines and neurot...
متن کاملRadionuclide labeling and evaluation of candidate radioligands for PET imaging of histone deacetylase in the brain.
Histone deacetylases (HDACs) regulate gene expression by inducing conformational changes in chromatin. Ever since the discovery of a naturally occurring HDAC inhibitor, trichostatin A (TSA) stimulated the recent development of suberoylanilide (SAHA, Zolinza®), HDAC has become an important molecular target for drug development. This has created the need to develop specific in vivo radioligands t...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Applied Sciences
سال: 2014
ISSN: 2076-3417
DOI: 10.3390/app4010066