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

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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.

Keywords: ATP hydrolysis; Alzheimer's disease; Blood-brain barrier; Carbon-11 Labeled Tracers; Constant of dissociation (Kd); Epilepsy; Inhibitors; Modulators; Multidrug resistance-associated proteins (MRP); Nucleotide-binding domains (NBDs); P-Glycoprotein Function; P-glycoprotein; P-gp tracers; PET; Parkinson's disease; Radiolabeling; Radiopharmaceuticals; Substrates; Tracer-kinetic modeling; [11C]/[18F]paclitaxel; [11C]Carvedilol; [11C]D617; [11C]Docetaxel; [11C]Elacridar; [11C]Laniquidar; [11C]MC18; [11C]Tariquidar; [11C]colchicine; [11C]daunorubicin; [11C]loperamide; [11C]verapamil; blood-brain barrier; cytochrome P450 (cyp 450); radiopharmaceuticals; tracer-kinetic modeling; β-amyloid peptide (Aβ)

Document Type: Research Article


Affiliations: University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging,Hanzeplein 1, 9713 GZ Groningen, The Netherlands.

Publication date: December 1, 2010


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