Publication

PET Imaging of ABC Transporters at the Blood-Brain Barrier

Garcia Varela, L., Mossel, P., Benadiba, M., Savolainen, H., Colabufo, N. A., Windhorst, A. D., Elsinga, P. H., van Waarde, A. & Luurtsema, G., 2020, (Accepted/In press) PET and SPECT of Neurobiological Systems. Dierckx, R., Otte, A., de Vries, E., van Waarde, A. & Lammertsma, A. (eds.). 2 ed. Springer Nature, 42 p.

Research output: Chapter in Book/Report/Conference proceedingChapterAcademicpeer-review

APA

Garcia Varela, L., Mossel, P., Benadiba, M., Savolainen, H., Colabufo, N. A., Windhorst, A. D., Elsinga, P. H., van Waarde, A., & Luurtsema, G. (Accepted/In press). PET Imaging of ABC Transporters at the Blood-Brain Barrier. In R. Dierckx, A. Otte, E. de Vries, A. van Waarde, & A. Lammertsma (Eds.), PET and SPECT of Neurobiological Systems (2 ed.). Springer Nature.

Author

Garcia Varela, Lara ; Mossel, Pascalle ; Benadiba, Marcel ; Savolainen, Heli ; Colabufo, Nicola Antonio ; Windhorst, Albert D. ; Elsinga, Philip H. ; van Waarde, Aren ; Luurtsema, Gert. / PET Imaging of ABC Transporters at the Blood-Brain Barrier. PET and SPECT of Neurobiological Systems. editor / Rudi Dierckx ; Andreas Otte ; Erik de Vries ; Aren van Waarde ; Adriaan Lammertsma. 2. ed. Springer Nature, 2020.

Harvard

Garcia Varela, L, Mossel, P, Benadiba, M, Savolainen, H, Colabufo, NA, Windhorst, AD, Elsinga, PH, van Waarde, A & Luurtsema, G 2020, PET Imaging of ABC Transporters at the Blood-Brain Barrier. in R Dierckx, A Otte, E de Vries, A van Waarde & A Lammertsma (eds), PET and SPECT of Neurobiological Systems. 2 edn, Springer Nature.

Standard

PET Imaging of ABC Transporters at the Blood-Brain Barrier. / Garcia Varela, Lara; Mossel, Pascalle; Benadiba, Marcel; Savolainen, Heli; Colabufo, Nicola Antonio; Windhorst, Albert D.; Elsinga, Philip H.; van Waarde, Aren; Luurtsema, Gert.

PET and SPECT of Neurobiological Systems. ed. / Rudi Dierckx; Andreas Otte; Erik de Vries; Aren van Waarde; Adriaan Lammertsma. 2. ed. Springer Nature, 2020.

Research output: Chapter in Book/Report/Conference proceedingChapterAcademicpeer-review

Vancouver

Garcia Varela L, Mossel P, Benadiba M, Savolainen H, Colabufo NA, Windhorst AD et al. PET Imaging of ABC Transporters at the Blood-Brain Barrier. In Dierckx R, Otte A, de Vries E, van Waarde A, Lammertsma A, editors, PET and SPECT of Neurobiological Systems. 2 ed. Springer Nature. 2020


BibTeX

@inbook{ad513c0abe1648a69b46b1a416472d53,
title = "PET Imaging of ABC Transporters at the Blood-Brain Barrier",
abstract = "The function of ATP-binding cassette (ABC) transporters at the blood-brain barrier (BBB) is to protect the brain from toxic compounds. Additionally,they play a crucial role in the onset and progression of several central nervous system (CNS) diseases as well as in drug resistance. Many compoundswere identified as substrates, inhibitors, inducers, or activators for ABC transporters, causing important drug-drug interactions. PET imaging representsan excellent tool for assessing the function and expression of ABC transporters. Over the last years, many PET tracers with different characteristicshave been developed, mainly for measuring P-glycoprotein (P-gp) function at the BBB. Although (R)-[11C]verapamil or [11C]N-desmethylloperamideare considered as the “gold standard” P-gp tracers, they have several drawbacks such as its high affinity to P-gp which limits their use for assessing P-gp increased function. Therefore, PET tracers with lower affinity to the transporter have been developed and studied in different species. The assessment of ABC transporters by PET imaging can provide new insight into the physiology and pathophysiology of different CNS diseases and may open new avenues for therapies. Moreover, PET can be used for screening the affinity of new entities toward various ABC transporters and thus enhance the development of CNS drugs.",
keywords = "POSITRON EMISSION TOMOGRAPHY, ABC Transporters, P-GLYCOPROTEIN, IMAGING, QUANTIFICATION, Kinetic modelling, Radiochemistry, Brain imaging, HUMAN BRAIN",
author = "{Garcia Varela}, Lara and Pascalle Mossel and Marcel Benadiba and Heli Savolainen and Colabufo, {Nicola Antonio} and Windhorst, {Albert D.} and Elsinga, {Philip H.} and {van Waarde}, Aren and Gert Luurtsema",
year = "2020",
language = "English",
isbn = "978-3-030-53175-1",
editor = "Rudi Dierckx and Andreas Otte and {de Vries}, Erik and {van Waarde}, Aren and Adriaan Lammertsma",
booktitle = "PET and SPECT of Neurobiological Systems",
publisher = "Springer Nature",
edition = "2",

}

RIS

TY - CHAP

T1 - PET Imaging of ABC Transporters at the Blood-Brain Barrier

AU - Garcia Varela, Lara

AU - Mossel, Pascalle

AU - Benadiba, Marcel

AU - Savolainen, Heli

AU - Colabufo, Nicola Antonio

AU - Windhorst, Albert D.

AU - Elsinga, Philip H.

AU - van Waarde, Aren

AU - Luurtsema, Gert

PY - 2020

Y1 - 2020

N2 - The function of ATP-binding cassette (ABC) transporters at the blood-brain barrier (BBB) is to protect the brain from toxic compounds. Additionally,they play a crucial role in the onset and progression of several central nervous system (CNS) diseases as well as in drug resistance. Many compoundswere identified as substrates, inhibitors, inducers, or activators for ABC transporters, causing important drug-drug interactions. PET imaging representsan excellent tool for assessing the function and expression of ABC transporters. Over the last years, many PET tracers with different characteristicshave been developed, mainly for measuring P-glycoprotein (P-gp) function at the BBB. Although (R)-[11C]verapamil or [11C]N-desmethylloperamideare considered as the “gold standard” P-gp tracers, they have several drawbacks such as its high affinity to P-gp which limits their use for assessing P-gp increased function. Therefore, PET tracers with lower affinity to the transporter have been developed and studied in different species. The assessment of ABC transporters by PET imaging can provide new insight into the physiology and pathophysiology of different CNS diseases and may open new avenues for therapies. Moreover, PET can be used for screening the affinity of new entities toward various ABC transporters and thus enhance the development of CNS drugs.

AB - The function of ATP-binding cassette (ABC) transporters at the blood-brain barrier (BBB) is to protect the brain from toxic compounds. Additionally,they play a crucial role in the onset and progression of several central nervous system (CNS) diseases as well as in drug resistance. Many compoundswere identified as substrates, inhibitors, inducers, or activators for ABC transporters, causing important drug-drug interactions. PET imaging representsan excellent tool for assessing the function and expression of ABC transporters. Over the last years, many PET tracers with different characteristicshave been developed, mainly for measuring P-glycoprotein (P-gp) function at the BBB. Although (R)-[11C]verapamil or [11C]N-desmethylloperamideare considered as the “gold standard” P-gp tracers, they have several drawbacks such as its high affinity to P-gp which limits their use for assessing P-gp increased function. Therefore, PET tracers with lower affinity to the transporter have been developed and studied in different species. The assessment of ABC transporters by PET imaging can provide new insight into the physiology and pathophysiology of different CNS diseases and may open new avenues for therapies. Moreover, PET can be used for screening the affinity of new entities toward various ABC transporters and thus enhance the development of CNS drugs.

KW - POSITRON EMISSION TOMOGRAPHY

KW - ABC Transporters

KW - P-GLYCOPROTEIN

KW - IMAGING

KW - QUANTIFICATION

KW - Kinetic modelling

KW - Radiochemistry

KW - Brain imaging

KW - HUMAN BRAIN

UR - https://www.springer.com/gp/book/9783030531751

M3 - Chapter

SN - 978-3-030-53175-1

BT - PET and SPECT of Neurobiological Systems

A2 - Dierckx, Rudi

A2 - Otte, Andreas

A2 - de Vries, Erik

A2 - van Waarde, Aren

A2 - Lammertsma, Adriaan

PB - Springer Nature

ER -

ID: 130268026