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Development of purine-derived (18)F-labeled pro-drug tracers for imaging of MRP1 activity with PET.

Galante, E; Okamura, T; Sander, K; Kikuchi, T; Okada, M; Zhang, MR; Robson, M; ... Arstad, E; + view all (2014) Development of purine-derived (18)F-labeled pro-drug tracers for imaging of MRP1 activity with PET. J Med Chem , 57 (3) pp. 1023-1032. 10.1021/jm401764a. Green open access

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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-[(18)F]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 non-invasive assessment of MRP1 activity in vivo.

Type: Article
Title: Development of purine-derived (18)F-labeled pro-drug tracers for imaging of MRP1 activity with PET.
Open access status: An open access version is available from UCL Discovery
DOI: 10.1021/jm401764a
Publisher version: http://dx.doi.org/10.1021/jm401764a
Language: English
Additional information: Copyright © 2014 American Chemical Society ACS AuthorChoice - Terms of Use CC-BY
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences > UCL Queen Square Institute of Neurology
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences > UCL Queen Square Institute of Neurology > Clinical and Experimental Epilepsy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Department of Imaging
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Experimental and Translational Medicine
UCL > Provost and Vice Provost Offices > UCL BEAMS
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences
UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry
URI: https://discovery.ucl.ac.uk/id/eprint/1418259
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