Blood brain barrier permeability of [11C]loperamide in humans under normal and impaired P-glycoprotein function
@inproceedings{Passchier2008BloodBB, 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}, year={2008} }
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10 Citations
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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…
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- 2015
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.
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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.
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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.
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