Abstract
Aiming to image NTS1 overexpressing tumors, the diarylpyrazole glycoconjugate 8, derived from the potent NTS1 antagonist SR142948A, was synthesized taking advantage of the palladium-catalyzed aminocarbonylation reaction. The glycoconjugate 8 displayed excellent affinity and selectivity toward NTS1. Radiosynthesis proceeded straightforwardly, obtaining [(18)F]8 with excellent stability and highly beneficial biodistribution in vivo as demonstrated by PET imaging in HT29 tumor-bearing nude mice. Thus, the tracer [(18)F]8 represents a highly promising candidate for PET imaging of NTS1-positive tumors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkynes / chemistry
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Animals
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Azides / chemistry
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Brain / diagnostic imaging
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Brain / metabolism
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Catalysis
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Cell Transformation, Neoplastic
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Chemistry Techniques, Synthetic
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Click Chemistry
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Fluorine Radioisotopes*
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Glycoconjugates / chemistry*
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HT29 Cells
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Humans
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Isotope Labeling
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Mice
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Microwaves
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Palladium / chemistry
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Positron-Emission Tomography / methods*
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Rats
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Receptors, Neurotensin / metabolism*
Substances
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Alkynes
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Azides
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Fluorine Radioisotopes
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Glycoconjugates
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Pyrazoles
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Receptors, Neurotensin
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neurotensin type 1 receptor
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Palladium