Carbon-11 labeled tracers for in vivo imaging P-glycoprotein function: kinetics, advantages and disadvantages.
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.
Luurtsema
G
G
University Medical Center Groningen, Department of Nuclear Medicine and Molecular Imaging, Hanzeplein 1, 9713 GZ Groningen, The Netherlands. g.luurtsema@ngmb.umcg.nl
Verbeek
G L
GL
Lubberink
M
M
Lammertsma
A A
AA
Dierckx
R
R
Elsinga
P
P
Windhorst
A D
AD
van Waarde
A
A
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D001812:Blood-Brain Barrier / Q000000981:diagnostic imaging / Q000378:metabolism; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism* / Q000473:pathology; D002247:Carbon Isotopes; D006801:Humans; D007700:Kinetics; D011849:Radioactive Tracers; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics*
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002247:Carbon Isotopes; D011849:Radioactive Tracers; D019275:Radiopharmaceuticals