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Blood-brain barrier P-glycoprotein function in Alzheimer's disease.
TLDR
Assessment of blood-brain barrier P-glycoprotein function in patients with Alzheimer's disease compared with age-matched healthy controls shows altered kinetics of (R)-[(11)C]verapamil in Alzheimer’s disease, similar to alterations seen in studies where P- glycoprotein is blocked by a pharmacological agent.
Limitations of Small Animal PET Imaging with [18F]FDDNP and FDG for Quantitative Studies in a Transgenic Mouse Model of Alzheimer’s Disease
TLDR
The authors could not detect regionally increased [18F]FDDNP binding and regionally decreased FDG binding in the brains of Tg2576 transgenic versus wild-type mice.
Pgp‐Mediated Interaction Between (R)‐[11C]Verapamil and Tariquidar at the Human Blood–Brain Barrier: A Comparison With Rat Data
TLDR
Both in humans and in rats, brain VT approached plateau levels at plasma tariquidar concentrations >1,000 ng/ml, however, Pgp inhibition in humans led to only a 2.7‐fold increase in brain VT relative to baseline scans (before administration of tarLiquidar) as compared with 11.0‐fold in rats.
Interaction of 11C-Tariquidar and 11C-Elacridar with P-Glycoprotein and Breast Cancer Resistance Protein at the Human Blood–Brain Barrier
TLDR
Both tracers were unable to visualize cerebral Pgp density, most likely because of insufficiently high binding affinities in relation to the low density of Pgp in human brain, and may find use as a new class of radiotracers to study the interplay of PGP and BCRP at the human BBB in limiting brain uptake of dual substrates.
Peripheral metabolism of (R)-[11C]verapamil in epilepsy patients
TLDR
Faster metabolism of (R)-[11C]verapamil in epilepsy patients may be caused by hepatic cytochrome P450 enzyme induction by antiepileptic drugs, and caution is warranted when using an averaged arterial input function derived from healthy volunteers for the analysis of patient data.
A Combined Accelerator Mass Spectrometry-Positron Emission Tomography Human Microdose Study with 14C- and 11C-Labelled Verapamil
TLDR
Combining AMS and PET microdosing allows long-term pharmacokinetic data along with information on drug tissue distribution to be acquired in the same subjects thus making it a promising approach to maximize data output from a single clinical study.
Assessment of P-Glycoprotein Transport Activity at the Human Blood–Retina Barrier with (R)‐11C-Verapamil PET
TLDR
A significant increase in (R)-11C-verapamil distribution to the retina duringABCB1 inhibition is found, which provides first in vivo evidence for ABCB1 transport activity at the human BRB.
A Pilot Study to Assess the Efficacy of Tariquidar to Inhibit P-glycoprotein at the Human Blood–Brain Barrier with (R)-11C-Verapamil and PET
TLDR
Tariquidar significantly increased brain penetration of (R)-11C-verapamil–derived activity due to increased influx and central P-gp inhibition appeared to be far from complete after the administered tariquidar dose.
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