Carbon-11 labeled tracers for in vivo imaging P-glycoprotein function: kinetics, advantages and disadvantages

• Published in: Current topics in medicinal chemistry Vol. 10; no. 17; p. 1820
• Main Authors: Luurtsema, G, Verbeek, G L, Lubberink, M, Lammertsma, A A, Dierckx, R, Elsinga, P, Windhorst, A D, van Waarde, A
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01-12-2010
• Subjects: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1 - antagonists & inhibitors; ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism; Biological Transport - drug effects; Blood-Brain Barrier - diagnostic imaging; Blood-Brain Barrier - metabolism; Brain - diagnostic imaging; Brain - metabolism; Brain - pathology; Carbon Isotopes; Humans; Kinetics; Radioactive Tracers; Radionuclide Imaging; Radiopharmaceuticals - chemistry; Radiopharmaceuticals - pharmacokinetics
• ISSN: 1873-4294
• DOI: 10.2174/156802610792928013

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.