• Corpus ID: 86725384

Blood brain barrier permeability of [11C]loperamide in humans under normal and impaired P-glycoprotein function

  title={Blood brain barrier permeability of [11C]loperamide in humans under normal and impaired P-glycoprotein function},
  author={Jan Passchier and Robert A. Comley and Cristian A. Salinas and Eugenii A. Rabiner and Roger N. Gunn and Vincent J. Cunningham and Alan A. Wilson and Sylvain Houle and Antony D. Gee and Marc Laruelle},
Drug interactions at the blood-brain barrier: fact or fantasy?
Retrospective Analysis of P-Glycoprotein–Mediated Drug-Drug Interactions at the Blood-Brain Barrier in Humans
To date, the in vitro–in vivo correlation (IVIVC) of P-glycoprotein (P-gp)–mediated drug-drug interaction (DDI) at the blood-brain barrier (BBB) in rats indicated that the cutoff value to
Proof-of-Concept Study of Drug Brain Permeability Between in Vivo Human Brain and an in Vitro iPSCs-Human Blood-Brain Barrier Model
The iPSC-hBBB model can be integrated in a flow scheme of CNS drug screening and potentially used to study species differences in BBB permeation, and a good correlation between in vitro and in vivo drug brain permeability is shown.
Current Concepts in Methadone Metabolism and Transport
  • E. Kharasch
  • Medicine, Biology
    Clinical pharmacology in drug development
  • 2017
It has now been unequivocally established that CYP2B6, not CYP3A4, is the principal determinant of methadone metabolism, clearance, elimination, and plasma concentrations in humans.
Modulation of P-glycoprotein at the Human Blood-Brain Barrier by Quinidine or Rifampin Treatment: A Positron Emission Tomography Imaging Study
It is concluded that rifampin, at its usual clinical dose, cannot be used to induce P-gp at the human BBB to a clinically meaningful extent and is unlikely to cause inadvertent BBB-inductive drug interactions.
Predicting the outer boundaries of P-glycoprotein (P-gp)-based drug interactions at the human blood-brain barrier based on rat studies.
The data suggest that clinically significant P-gp based drug interactions at the human BBB are possible for P- gp substrates highly excluded from the brain and should be investigated using noninvasive approaches.
Cyclosporine-inhibitable Cerebral Drug Transport Does Not Influence Clinical Methadone Pharmacodynamics
The result does not support a role for cyclosporine-inhibitable transporters mediating methadone brain access and biodistribution.
P-glycoprotein-based loperamide-cyclosporine drug interaction at the rat blood-brain barrier: prediction from in vitro studies and extrapolation to humans.
The rat is a promising model to predict P-gp based DDI at the human blood-brain barrier (BBB) and the potency (EC(50)) of CsA to inhibit rat BBB P- gp could be predicted from in vitro studies in MDRI-transfected cells.
Pgp‐Mediated Interaction Between (R)‐[11C]Verapamil and Tariquidar at the Human Blood–Brain Barrier: A Comparison With Rat Data
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.