Development of Purine-Derived18F-Labeled Pro-drug Tracers for Imaging of MRP1 Activity with PET

Article

Galante, E., Okamura, Toshimitsu, Sande, Kerstin, Kikuchi, Tatsuya, Okada, Maki, Zhang, Ming-Rong, Robson, Mathew, Badar, Adam, Lythgoe, Mark, Koepp, Matthias and Årstad, Erik 2014. Development of Purine-Derived18F-Labeled Pro-drug Tracers for Imaging of MRP1 Activity with PET. Journal of Medicinal Chemistry. 57 (3), pp. 1023-1032. https://doi.org/10.1021/jm401764a
AuthorsGalante, E., Okamura, Toshimitsu, Sande, Kerstin, Kikuchi, Tatsuya, Okada, Maki, Zhang, Ming-Rong, Robson, Mathew, Badar, Adam, Lythgoe, Mark, Koepp, Matthias and Årstad, Erik
Abstract

Multidrug resistance-associated protein 1 (MRP1) is a drug efflux transporter that has been implicated in the pathology of several neurological diseases and is associated with development of multidrug resistance. To enable measurement of MRP1 function in the living brain, a series of 6-halopurines decorated with fluorinated side chains have been synthesized and evaluated as putative pro-drug tracers. The tracers were designed to undergo conjugation with glutathione within the brain and hence form the corresponding MRP1 substrate tracers in situ.
6-Bromo-7-(2-[18F]fluoroethyl)purine showed good brain uptake and rapid metabolic conversion. Dynamic PET imaging demonstrated a marked difference in brain clearance rates between wild-type and mrp1 knockout mice, suggesting that the tracer can allow noninvasive assessment of MRP1 activity in vivo.

JournalJournal of Medicinal Chemistry
Journal citation57 (3), pp. 1023-1032
ISSN0022-2623
Year2014
PublisherAmerican Chemical Society (ACS)
Digital Object Identifier (DOI)https://doi.org/10.1021/jm401764a
Web address (URL)https://doi.org/10.1021/jm401764a
Publication dates
Print23 Jan 2014
Publication process dates
Deposited18 Aug 2017
Accepted01 Jan 2014
Copyright information© 2014 American Chemical Society
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