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.

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