pgp - publications

Predict more pgp - ligand interactions now!

1. Mol Imaging Biol. 2012 Apr 3. [Epub ahead of print]

P-Glycoprotein Function at the Blood-Brain Barrier: Effects of Age and Gender.

van Assema DM, Lubberink M, Boellaard R, Schuit RC, Windhorst AD, Scheltens P,
Lammertsma AA, van Berckel BN.

Department of Nuclear Medicine & PET Research, VU University Medical Center, PO
Box 7057, 1007 MB, Amsterdam, the Netherlands,

PURPOSE: P-glycoprotein (Pgp) is an efflux transporter involved in transport of
several compounds across the blood-brain barrier (BBB). Loss of Pgp function with
increasing age may be involved in the development of age-related disorders, but
this may differ between males and females. Pgp function can be quantified in vivo
using (R)-[(11)C]verapamil and positron emission tomography. The purpose of this
study was to assess global and regional effects of both age and gender on BBB Pgp
function. PROCEDURES: Thirty-five healthy men and women in three different age
groups were included. Sixty minutes dynamic (R)-[(11)C]verapamil scans with
metabolite-corrected arterial plasma input curves were acquired. Grey matter
time-activity curves were fitted to a validated constrained two-tissue
compartment plasma input model, providing the volume of distribution (V (T)) of
(R)-[(11)C]verapamil as outcome measure. RESULTS: Increased V (T) of
(R)-[(11)C]verapamil with aging was found in several large brain regions in men.
Young and elderly women showed comparable V (T) values. Young women had higher V
(T) compared with young men. CONCLUSIONS: Decreased BBB Pgp is found with aging;
however, effects of age on BBB Pgp function differ between men and women.

PMID: 22476967 [PubMed - as supplied by publisher]