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1 - 2 of 2 for ""[11C]daunorubicin""
Imaging of P-glycoprotein Function and Expression to Elucidate Mechanisms of Pharmacoresistance in Epilepsy
The issue of pharmacoresistance in epilepsy has received considerable attention in recent years and a number of plausible hypotheses have been proposed. Of these the so-called transporter hypothesis is the most extensively researched and documented. This hypothesis assumes that refractory epilepsy is associated with a localised over-expression of drug transporter proteins such as P-glycoprotein (Pgp) in the region of the epileptic focus which actively extrudes antiepileptic drugs (AEDs) from their intended site of action. However although this hypothesis has biological plausibility there is no clinical evidence to support the assertion that AEDs are sufficiently strong substrates for transportermediated extrusion from the brain. The use of modern brain imaging techniques to determine Pgp function in patients with refractory epilepsy has started only recently and may ultimately determine whether increased expression and function of Pgp or other efflux transporters are involved in AED resistance.
Carbon-11 Labeled Tracers for In Vivo Imaging of 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.