Functional imaging of P-glycoprotein in the blood-brain barrier with PET: State of the art

N. H. Hendrikse, G. Luurtsema, B. N.M. Van Berckel, E. J.F. Franssen, A. A. Lammertsma

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

Abstract

The blood-brain barrier (BBB) is the main barrier between blood and brain. Its purpose is to maintain homeostasis in and protection of the central nervous system. Therefore, under normal physiological conditions, the BBB is impermeable for endotoxins, but also for exotoxins like drugs. In the endothelial cells of the BBB, different active influx, but also active drug efflux transporters are presents. An example of drug efflux pumps is P-glycoprotein (P-gp) drug efflux pumps, which are encoded by MDR1 genes in humans. A different P-gp expression in the blood-brain barrier can play a role in the aetiology of several brain disorders. For this reason, there is a need to develop an assay for the quantification P-gp functionality in the BBB. We discuss, the relationship of P-gp and brain pathology and the involvement of age in loss of P-gp function. Furthermore, drugs treatment of brain diseases like Alzheimers's disease and Parkinson's disease are often not effective. Therefore, we discuss the relationship between P-gp and drug availability. In this chapter, an overview is given in the use of positron emission tomography as a tool for measuring P-gp function in the area of neurology, neurophysiology and pharmacology.

Original languageEnglish
Title of host publicationHandbook of Neurochemistry and Molecular Neurobiology
Subtitle of host publicationNeural Membranes and Transport
PublisherSpringer US
Pages99-107
Number of pages9
ISBN (Print)9780387303468
DOIs
Publication statusPublished - 1 Dec 2007

Cite this

Hendrikse, N. H., Luurtsema, G., Van Berckel, B. N. M., Franssen, E. J. F., & Lammertsma, A. A. (2007). Functional imaging of P-glycoprotein in the blood-brain barrier with PET: State of the art. In Handbook of Neurochemistry and Molecular Neurobiology: Neural Membranes and Transport (pp. 99-107). Springer US. https://doi.org/10.1007/978-0-387-30380-2_5
Hendrikse, N. H. ; Luurtsema, G. ; Van Berckel, B. N.M. ; Franssen, E. J.F. ; Lammertsma, A. A. / Functional imaging of P-glycoprotein in the blood-brain barrier with PET : State of the art. Handbook of Neurochemistry and Molecular Neurobiology: Neural Membranes and Transport. Springer US, 2007. pp. 99-107
@inbook{9ebd87e9b4d64e029ae7dc884182ffd2,
title = "Functional imaging of P-glycoprotein in the blood-brain barrier with PET: State of the art",
abstract = "The blood-brain barrier (BBB) is the main barrier between blood and brain. Its purpose is to maintain homeostasis in and protection of the central nervous system. Therefore, under normal physiological conditions, the BBB is impermeable for endotoxins, but also for exotoxins like drugs. In the endothelial cells of the BBB, different active influx, but also active drug efflux transporters are presents. An example of drug efflux pumps is P-glycoprotein (P-gp) drug efflux pumps, which are encoded by MDR1 genes in humans. A different P-gp expression in the blood-brain barrier can play a role in the aetiology of several brain disorders. For this reason, there is a need to develop an assay for the quantification P-gp functionality in the BBB. We discuss, the relationship of P-gp and brain pathology and the involvement of age in loss of P-gp function. Furthermore, drugs treatment of brain diseases like Alzheimers's disease and Parkinson's disease are often not effective. Therefore, we discuss the relationship between P-gp and drug availability. In this chapter, an overview is given in the use of positron emission tomography as a tool for measuring P-gp function in the area of neurology, neurophysiology and pharmacology.",
author = "Hendrikse, {N. H.} and G. Luurtsema and {Van Berckel}, {B. N.M.} and Franssen, {E. J.F.} and Lammertsma, {A. A.}",
year = "2007",
month = "12",
day = "1",
doi = "10.1007/978-0-387-30380-2_5",
language = "English",
isbn = "9780387303468",
pages = "99--107",
booktitle = "Handbook of Neurochemistry and Molecular Neurobiology",
publisher = "Springer US",

}

Hendrikse, NH, Luurtsema, G, Van Berckel, BNM, Franssen, EJF & Lammertsma, AA 2007, Functional imaging of P-glycoprotein in the blood-brain barrier with PET: State of the art. in Handbook of Neurochemistry and Molecular Neurobiology: Neural Membranes and Transport. Springer US, pp. 99-107. https://doi.org/10.1007/978-0-387-30380-2_5

Functional imaging of P-glycoprotein in the blood-brain barrier with PET : State of the art. / Hendrikse, N. H.; Luurtsema, G.; Van Berckel, B. N.M.; Franssen, E. J.F.; Lammertsma, A. A.

Handbook of Neurochemistry and Molecular Neurobiology: Neural Membranes and Transport. Springer US, 2007. p. 99-107.

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

TY - CHAP

T1 - Functional imaging of P-glycoprotein in the blood-brain barrier with PET

T2 - State of the art

AU - Hendrikse, N. H.

AU - Luurtsema, G.

AU - Van Berckel, B. N.M.

AU - Franssen, E. J.F.

AU - Lammertsma, A. A.

PY - 2007/12/1

Y1 - 2007/12/1

N2 - The blood-brain barrier (BBB) is the main barrier between blood and brain. Its purpose is to maintain homeostasis in and protection of the central nervous system. Therefore, under normal physiological conditions, the BBB is impermeable for endotoxins, but also for exotoxins like drugs. In the endothelial cells of the BBB, different active influx, but also active drug efflux transporters are presents. An example of drug efflux pumps is P-glycoprotein (P-gp) drug efflux pumps, which are encoded by MDR1 genes in humans. A different P-gp expression in the blood-brain barrier can play a role in the aetiology of several brain disorders. For this reason, there is a need to develop an assay for the quantification P-gp functionality in the BBB. We discuss, the relationship of P-gp and brain pathology and the involvement of age in loss of P-gp function. Furthermore, drugs treatment of brain diseases like Alzheimers's disease and Parkinson's disease are often not effective. Therefore, we discuss the relationship between P-gp and drug availability. In this chapter, an overview is given in the use of positron emission tomography as a tool for measuring P-gp function in the area of neurology, neurophysiology and pharmacology.

AB - The blood-brain barrier (BBB) is the main barrier between blood and brain. Its purpose is to maintain homeostasis in and protection of the central nervous system. Therefore, under normal physiological conditions, the BBB is impermeable for endotoxins, but also for exotoxins like drugs. In the endothelial cells of the BBB, different active influx, but also active drug efflux transporters are presents. An example of drug efflux pumps is P-glycoprotein (P-gp) drug efflux pumps, which are encoded by MDR1 genes in humans. A different P-gp expression in the blood-brain barrier can play a role in the aetiology of several brain disorders. For this reason, there is a need to develop an assay for the quantification P-gp functionality in the BBB. We discuss, the relationship of P-gp and brain pathology and the involvement of age in loss of P-gp function. Furthermore, drugs treatment of brain diseases like Alzheimers's disease and Parkinson's disease are often not effective. Therefore, we discuss the relationship between P-gp and drug availability. In this chapter, an overview is given in the use of positron emission tomography as a tool for measuring P-gp function in the area of neurology, neurophysiology and pharmacology.

UR - http://www.scopus.com/inward/record.url?scp=84900925619&partnerID=8YFLogxK

U2 - 10.1007/978-0-387-30380-2_5

DO - 10.1007/978-0-387-30380-2_5

M3 - Chapter

SN - 9780387303468

SP - 99

EP - 107

BT - Handbook of Neurochemistry and Molecular Neurobiology

PB - Springer US

ER -

Hendrikse NH, Luurtsema G, Van Berckel BNM, Franssen EJF, Lammertsma AA. Functional imaging of P-glycoprotein in the blood-brain barrier with PET: State of the art. In Handbook of Neurochemistry and Molecular Neurobiology: Neural Membranes and Transport. Springer US. 2007. p. 99-107 https://doi.org/10.1007/978-0-387-30380-2_5