Skip to content
2000
Volume 22, Issue 38
  • ISSN: 1381-6128
  • E-ISSN: 1873-4286

Abstract

P-glycoprotein function is associated with a number of neurodegenerative and psychiatric diseases as well as with pharmacoresistance to for example antiepileptic drugs. The ability to measure P-gp function in vivo would allow for an increased understanding of the mechanisms of disease and treatment. This review assesses the various approaches to in vivo quantification of P-gp function using currently available P-gp tracers and PET in humans. First, the use of compartment models, and their interpretation in terms of P-gp function at the blood-brain barrier, is discussed. Then, the methods that have been used to quantify PET data of the P-gp tracers [11C]verapamil, [11C]N-desmetyl-loperamide (dLop), [11C]laniquidar, [11C]phenytoin, [11C]tariquidar and [11C]elacridar are reviewed. In summary, the extraction of P-gp substrate PET tracers, which is their plasma to tissue rate constant K1 corrected for variations in regional cerebral blood flow, is generally considered to be the preferred measure of P-gp function.

Loading

Article metrics loading...

/content/journals/cpd/10.2174/1381612822666160804093852
2016-10-01
2025-05-10
Loading full text...

Full text loading...

/content/journals/cpd/10.2174/1381612822666160804093852
Loading

  • Article Type:
    Research Article
Keyword(s): blood-brain barrier; P-glycoprotein; PET; quantification; tracer kinetics
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test