title: Radiopharmaceuticals for assessing ABC transporters at the blood-brain barrier.
abstract: 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.
authors: Department of Radiology & Nuclear Medicine, VU University Medical Center Amsterdam, The Netherlands.
authors: R M
authors: RM
authors: Raaphorst
authors: A D
authors: AD
authors: Windhorst
authors: P H
authors: PH
authors: Elsinga
authors: N A
authors: NA
authors: Colabufo
authors: A A
authors: AA
authors: Lammertsma
authors: G
authors: G
authors: Luurtsema
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D000818:Animals; D001812:Blood-Brain Barrier / Q000000981:diagnostic imaging* / Q000378:metabolism* / Q000502:physiology; D006801:Humans; D019636:Neurodegenerative Diseases / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D049268:Positron-Emission Tomography / Q000379:methods / Q000639:trends; D019275:Radiopharmaceuticals
chemical_list: D018528:ATP-Binding Cassette Transporters; D019275:Radiopharmaceuticals