(18)F-FCWAY, a serotonin 1A receptor radioligand, is a substrate for efflux transport at the human blood-brain barrier

• Published in: NeuroImage (Orlando, Fla.) Vol. 138; p. 134
• Main Authors: Liow, Jeih-San, Zoghbi, Sami S, Hu, Shuo, Hall, Matthew D, Hines, Christina S, Shetty, H Umesha, Araneta, Maria D, Page, Emily M, Pike, Victor W, Kreisl, William C, Herscovitch, Peter, Gottesman, Michael M, Theodore, William H, Innis, Robert B
• Format: Journal Article
• Language: English
• Published: United States 01.09.2016
• Subjects: Adult; ATP Binding Cassette Transporter, Subfamily B - metabolism; ATP Binding Cassette Transporter, Subfamily G, Member 2 - metabolism; Blood-Brain Barrier - metabolism; Capillary Permeability - physiology; Cyclohexanes - pharmacokinetics; Female; Humans; Male; Multidrug Resistance-Associated Proteins - metabolism; Neoplasm Proteins - metabolism; Piperazines - pharmacokinetics; Positron-Emission Tomography - methods; Radiopharmaceuticals - pharmacokinetics; Receptor, Serotonin, 5-HT1A - metabolism; Reproducibility of Results; Sensitivity and Specificity; 5-HT(1A); P-gp; Blood brain barrier; Efflux transporter; PET

Efflux transporters at the blood-brain barrier can decrease the entry of drugs and increase the removal of those molecules able to bypass the transporter. We previously hypothesized that (18)F-FCWAY, a radioligand for the serotonin 5-HT1A receptor, is a weak substrate for permeability glycoprotein (...