PMID: 20645911Jul 22, 2010Paper

PET imaging of MRP1 function in the living brain: method development and future perspectives

Current Topics in Medicinal Chemistry
Toshimitsu OkamuraToshiaki Irie

Abstract

Multidrug resistance-associated protein 1 (MRP1) functions as a primary active transporter utilizing energy from ATP hydrolysis. In the central nervous system (CNS), MRP1 plays an important role in limiting the permeation of xenobiotic and endogenous substrates across the blood-brain and blood-cerebrospinal fluid barriers, and across brain parenchymal cells. While MRP1 contributes to minimizing the neurotoxic effects of drugs, it may also restrict the distribution of drugs for the treatment of CNS diseases. Moreover, neurodegenerative disease may be associated with abnormal expression of efflux transporters in the brain. Noninvasive measurement of MRP1 function will therefore be useful for directly evaluating the effect of modulators on enhancing the penetration of drugs into the brain and for examining the pathophysiological role of MRP1 in the brain. Positron emission tomography (PET) is a powerful molecular imaging technique. While several PET probes have been proposed for imaging function of the efflux transporter P-glycoprotein, few reports discuss the probes for imaging MRP1 function in the brain. Ideally, brain radioactivity should consist of a single radioactive compound that is selectively transported by the efflux tra...Continue Reading

Citations

Oct 2, 2012·CNS Drugs·Yumiko AkamineTsukasa Uno
Apr 2, 2013·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Cristina BolzatiNicola Antonio Colabufo
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Tatsuya KikuchiToshiaki Irie
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Thomas WanekOliver Langer
May 10, 2017·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Massoud SaidijamSimon G Patching

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