Carbon-11 Labeled Tracers for In Vivo Imaging of P-Glycoprotein Function: Kinetics, Advantages and Disadvantages

Geert Luurtsema, Joost Verbeek, Mark Lubberink, Adriaan A. Lammertsma, Rudi Dierckx, Philippus Elsinga, Albert D. Windhorst, Aren van Waarde

Research output: Contribution to journalReview articlepeer-review

18 Citations (Scopus)

Abstract

P-glycoprotein (P-gp) is a drug efflux transporter with broad substrate specificity localized in the blood-brain barrier and in several peripheral organs. In order to understand the role of P-gp in physiological and patho-physiological conditions, several carbon-11 labelled P-gp tracers have been developed and validated.

This review provides an overview of the spectrum of radiopharmaceuticals that is available for this purpose. A short overview of the physiology of the blood-brain barrier in health and disease is also provided. Tracer kinetic modelling for quantitative analysis of P-gp function and expression is highlighted, and the advantages and disadvantages of the various tracers are discussed.

Original languageEnglish
Pages (from-to)1820-1833
Number of pages14
JournalCurrent topics in medicinal chemistry
Volume10
Issue number17
DOIs
Publication statusPublished - Dec-2010

Keywords

  • PET
  • P-glycoprotein
  • blood-brain barrier
  • radiopharmaceuticals
  • tracer-kinetic modeling
  • BLOOD-BRAIN-BARRIER
  • POSITRON-EMISSION-TOMOGRAPHY
  • MULTIDRUG-RESISTANCE
  • PARKINSONS-DISEASE
  • ALZHEIMERS-DISEASE
  • BIOLOGICAL EVALUATION
  • RECEPTOR-BINDING
  • PET RADIOTRACER
  • TRANSPORT
  • RAT

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