@article{oai:repo.qst.go.jp:00046984, author = {Galante, Eva and Okamura, Toshimitsu and Sander, Kerstin and Kikuchi, Tatsuya and Okada, Maki and Zhang, Ming-Rong and Robson, Mathew and Badar, Adam and Lythgoe, Mark and Koepp, Matthias and Årstad, Erik and 岡村 敏充 and 菊池 達矢 and 岡田 真希 and 張 明栄}, issue = {3}, journal = {Journal of Medicinal Chemistry}, month = {Feb}, note = {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.}, pages = {1023--1032}, title = {Development of Purine-Derived 18F‑Labeled Pro-drug Tracers for Imaging of MRP1 Activity with PET}, volume = {57}, year = {2014} }