Functional imaging of P-glycoprotein in the blood-brain barrier with PET: State of the art

N. H. Hendrikse, G. Luurtsema, B. N.M. Van Berckel, E. J.F. Franssen, A. A. Lammertsma

Research output: Chapter in Book/Report/Conference proceedingChapterAcademicpeer-review


The blood-brain barrier (BBB) is the main barrier between blood and brain. Its purpose is to maintain homeostasis in and protection of the central nervous system. Therefore, under normal physiological conditions, the BBB is impermeable for endotoxins, but also for exotoxins like drugs. In the endothelial cells of the BBB, different active influx, but also active drug efflux transporters are presents. An example of drug efflux pumps is P-glycoprotein (P-gp) drug efflux pumps, which are encoded by MDR1 genes in humans. A different P-gp expression in the blood-brain barrier can play a role in the aetiology of several brain disorders. For this reason, there is a need to develop an assay for the quantification P-gp functionality in the BBB. We discuss, the relationship of P-gp and brain pathology and the involvement of age in loss of P-gp function. Furthermore, drugs treatment of brain diseases like Alzheimers's disease and Parkinson's disease are often not effective. Therefore, we discuss the relationship between P-gp and drug availability. In this chapter, an overview is given in the use of positron emission tomography as a tool for measuring P-gp function in the area of neurology, neurophysiology and pharmacology.

Original languageEnglish
Title of host publicationHandbook of Neurochemistry and Molecular Neurobiology
Subtitle of host publicationNeural Membranes and Transport
PublisherSpringer US
Number of pages9
ISBN (Print)9780387303468
Publication statusPublished - 1 Dec 2007

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