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Radiopharmaceuticals for Assessing ABC Transporters at the Blood-Brain Barrier

Raaphorst, R. M., Windhorst, A. D., Elsinga, P. H., Colabufo, N. A., Lammertsma, A. A. & Luurtsema, G., Apr-2015, In : Clinical Pharmacology & Therapeutics. 97, 4, p. 362-371 10 p.

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  • Radiopharmaceuticals for Assessing ABC Transporters at the Blood-Brain Barrier

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DOI

ABC transporters protect the brain by transporting neurotoxic compounds from the brain back into the blood. P-glycoprotein (P-gp) is the most investigated ABC (efflux) transporter, as it is implicated in neurodegenerative diseases such as Alzheimer's disease. Altered function of P-gp can be studied in vivo, using Positron Emission Tomography (PET). To date, several radiopharmaceuticals have been developed to image P-gp function in vivo. So far, attempts to image expression levels of P-gp using radiolabeled P-gp inhibitors have not been successful. Improved knowledge of compound behavior toward P-gp from in vitro studies should increase predictability of in vivo outcome.

Original languageEnglish
Pages (from-to)362-371
Number of pages10
JournalClinical Pharmacology & Therapeutics
Volume97
Issue number4
Publication statusPublished - Apr-2015

    Keywords

  • POSITRON-EMISSION-TOMOGRAPHY, CANCER RESISTANCE PROTEIN, P-GLYCOPROTEIN FUNCTION, DRUG EFFLUX TRANSPORTERS, IN-VIVO EVALUATION, MULTIDRUG-RESISTANCE, PARKINSONS-DISEASE, TARIQUIDAR XR9576, PET, INHIBITOR

ID: 20107258