Interaction of 11C-tariquidar and 11C-elacridar with P-glycoprotein and breast cancer resistance protein at the human blood-brain barrier

• Published in: The Journal of nuclear medicine (1978) Vol. 54; no. 8; p. 1181
• Main Authors: Bauer, Martin, Karch, Rudolf, Zeitlinger, Markus, Stanek, Johann, Philippe, Cécile, Wadsak, Wolfgang, Mitterhauser, Markus, Jäger, Walter, Haslacher, Helmuth, Müller, Markus, Langer, Oliver
• Format: Journal Article
• Language: English
• Published: United States 01.08.2013
• Subjects: Acridines - metabolism; Adult; ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters - metabolism; Blood-Brain Barrier - diagnostic imaging; Blood-Brain Barrier - metabolism; Carbon Radioisotopes; Humans; Male; Neoplasm Proteins - metabolism; Positron-Emission Tomography; Protein Binding; Quinolines - metabolism; Tetrahydroisoquinolines - metabolism; 11C-elacridar; P-glycoprotein; blood-brain barrier; breast cancer resistance protein; 11C-tariquidar
• ISSN: 1535-5667; 0161-5505; 1535-5667
• DOI: 10.2967/jnumed.112.118232

The adenosine triphosphate-binding cassette transporters P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) are 2 major gatekeepers at the blood-brain barrier (BBB) that restrict brain distribution of several clinically used drugs. In this study, we investigated the suitability of the...