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Kinetic models for measuring P-glycoprotein function at the blood-brain barrier with Positron Emission Tomography.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Surgical Sciences, Radiology.
2016 (English)In: Current pharmaceutical design, ISSN 1381-6128, E-ISSN 1873-4286Article in journal (Refereed) Epub ahead of print
Abstract [en]

P-glycoprotein function is associated with a number of neurodegenerative and psychiatric diseases as well as with pharmacoresistance to for example antiepileptic drugs. The ability to measure P-gp function in vivo would allow for an increased understanding of the mechanisms of disease and treatment. This review assesses the various approaches to in vivo quantification of P-gp function using currently available P-gp tracers and PET in humans. First, the use of compartment models, and their interpretation in terms of P-gp function at the blood-brain barrier, is discussed. Then, the methods that have been used to quantify PET data of the P-gp tracers [11C]verapamil, [11C]N-desmetyl-loperamide (dLop), [11C]laniquidar, [11C]phenytoin, [11C]tariquidar and [11C]elacridar are reviewed. In summary, the extraction of P-gp substrate PET tracers, which is their plasma to tissue rate constant K1 corrected for variations in regional cerebral blood flow, is generally considered to be the preferred measure of P-gp function.

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Medical and Health Sciences
URN: urn:nbn:se:uu:diva-312407PubMedID: 27494063OAI: oai:DiVA.org:uu-312407DiVA: diva2:1063228
Available from: 2017-01-09 Created: 2017-01-09 Last updated: 2017-01-09

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