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Biological Evaluation ofl-Tyrosine Labelled withfac-[99mTc(CO)3]+at apara-OH-Coupled 2,3-Diaminopropionic Acid Based Chelator


Felber, Michael; Bauwens, Matthias; Imstepf, Sebastian; Fox, Thomas; Mottaghy, Felix M; Alberto, Roger (2017). Biological Evaluation ofl-Tyrosine Labelled withfac-[99mTc(CO)3]+at apara-OH-Coupled 2,3-Diaminopropionic Acid Based Chelator. European Journal of Inorganic Chemistry, 2017(12):1772-1777.

Abstract

Radiolabeled amino acids as metabolic tracers are increasingly important for imaging and therapy applications. There are only a few reports on 99mTc-labeled amino acids that have been evaluated in vivo. In this work we coupled a small and highly potent chelator for the fac-[99mTc(CO)3]+ core to l-tyrosine through a poly(ethylene glycol) linker and investigated the in vivo biodistribution of the 99mTc-labeled l-tyrosine derivative. In vivo evaluation and biodistribution in mice bearing C6-tumor xenografts revealed little tumor and pancreas uptake. The microSPECT images showed rapid clearance from the blood pool. Fast uptake into the gallbladder and an extended residence time makes this labeled tyrosine suitable for gallbladder imaging and associated dysfunctions.

Abstract

Radiolabeled amino acids as metabolic tracers are increasingly important for imaging and therapy applications. There are only a few reports on 99mTc-labeled amino acids that have been evaluated in vivo. In this work we coupled a small and highly potent chelator for the fac-[99mTc(CO)3]+ core to l-tyrosine through a poly(ethylene glycol) linker and investigated the in vivo biodistribution of the 99mTc-labeled l-tyrosine derivative. In vivo evaluation and biodistribution in mice bearing C6-tumor xenografts revealed little tumor and pancreas uptake. The microSPECT images showed rapid clearance from the blood pool. Fast uptake into the gallbladder and an extended residence time makes this labeled tyrosine suitable for gallbladder imaging and associated dysfunctions.

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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Uncontrolled Keywords:Inorganic Chemistry
Language:English
Date:2017
Deposited On:09 Feb 2018 08:03
Last Modified:19 Aug 2018 13:49
Publisher:Wiley-Blackwell Publishing, Inc.
ISSN:1434-1948
Funders:COST program CM1105 with project C13.0080
OA Status:Closed
Publisher DOI:https://doi.org/10.1002/ejic.201601316

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