Published in:
Open Access
01-11-2021 | Verapamil | Image of the Month
Evaluation of P-glycoprotein function at the blood–brain barrier using [18F]MC225-PET
Authors:
Pascalle Mossel, Lara Garcia Varela, Wejdan M. Arif, Chris W. J. van der Weijden, Hendrikus H. Boersma, Antoon T. M. Willemsen, Ronald Boellaard, Philip H. Elsinga, Ronald J. H. Borra, Nicola A. Colabufo, Jun Toyohara, Peter Paul de Deyn, Rudi A. J. O. Dierckx, Adriaan A. Lammertsma, Anna L. Bartels, Gert Luurtsema
Published in:
European Journal of Nuclear Medicine and Molecular Imaging
|
Issue 12/2021
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Excerpt
P-glycoprotein (P-gp) is an ATP-dependent efflux transporter located at the blood–brain barrier (BBB), involved in the transport of a variety of neurotoxic substances out of the brain. Alterations in P-gp function play an essential role in the pathophysiological mechanisms underlying neurodegenerative disorders. The most widely used tracer to measure BBB P-gp function in vivo is
(R)-[
11C]verapamil [
1]. However,
(R)-[
11C]verapamil is an avid P-gp substrate, and its low uptake hampers the measurement of increases in P-gp function. In order to overcome this limitation, [
18F]MC225 was developed as a novel PET tracer to measure P-gp function in vivo. [
18F]MC225 is a weaker P-gp substrate and has shown higher brain uptake than
(R)-[
11C]verapamil at baseline in preclinical studies [
2]. This may facilitate the evaluation of both increases and decreases in P-gp function. In addition, the longer half-life of fluorine-18 enables the use of [
18F]MC225 in centers without an onsite cyclotron. …
