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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.
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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/18Fpaclitaxel; 11CCarvedilol; 11CD617; 11CDocetaxel; 11CElacridar; 11CLaniquidar; 11CMC18; 11CTariquidar; 11Ccolchicine; 11Cdaunorubicin; 11Cloperamide; 11Cverapamil; 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: 2010-12-01

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