量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum and Radiological Science and Technology.
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Multidrug resistance-associated protein 1 (MRP1) is a member of the adenosine triphosphate–binding cassette superfamily of transporters and plays an important role in limiting the permeation of xenobiotics and exporting endogenous substances across the blood-brain and blood-cerebrospinal fluid barriers, and across brain parenchymal cells in the central nervous system. In addition to multidrug resistance, changes in activity or expression of cerebral MRP1 occur in several brain diseases. Therefore, noninvasive and quantitative assessment of MRP1 activity in the brain is valuable for investigating the changes in MRP1 related to brain diseases, towards an understanding of the underlying molecular mechanisms. In this chapter, we will focus on 6-bromo-7-[11C]methylpurine for imaging MRP1 activity, as well as the concept of the metabolite extrusion method (MEM) for measuring efflux transporter activity. Several positron emission tomography (PET) and single-photon emission computed tomography (SPECT) imaging studies of MRPs activity are also reviewed. Finally, we discuss our recent findings regarding the contribution of Mrp1 in brain parenchymal cells to tracer efflux, and the sensitivity of 6-bromo-7-[11C]methylpurine for measuring MRP1 activity.
PET and SPECT of Neurobiological Systems
