Assessment of Regional Differences in Tariquidar-Induced P-Glycoprotein Modulation at the Human Blood–Brain Barrier

• Published in: Journal of cerebral blood flow and metabolism Vol. 30; no. 3; pp. 510 - 515
• Main Authors: Bauer, Martin, Karch, Rudolf, Neumann, Friederike, Wagner, Claudia C, Kletter, Kurt, Müller, Markus, Löscher, Wolfgang, Zeitlinger, Markus, Langer, Oliver
• Format: Journal Article
• Language: English
• Published: London, England SAGE Publications 01.03.2010; Nature Publishing Group; Sage Publications Ltd
• Subjects: Adult; ATP Binding Cassette Transporter, Subfamily B, Member 1 - physiology; Biological and medical sciences; Blood-Brain Barrier - drug effects; Blood-Brain Barrier - physiology; Brain - diagnostic imaging; Brief Communication; Calcium Channel Blockers - metabolism; Drug Resistance, Multiple - drug effects; Epilepsy - chemically induced; Epilepsy - physiopathology; Humans; Image Processing, Computer-Assisted; Infusions, Intravenous; Investigative techniques, diagnostic techniques (general aspects); Male; Medical sciences; Nervous system; Neurology; Positron-Emission Tomography; Quinolines - pharmacology; Ultrasonic investigative techniques; Vascular diseases and vascular malformations of the nervous system; Verapamil - metabolism; P-glycoprotein; blood–brain barrier; tariquidar; positron emission tomography (PET); regional; (R)-[11C]verapamil; Antineoplastic agent; Human; blood-brain barrier; Nervous system diseases; regional tariquidar; Tariquidar; Calcium antagonist; Glycoprotein; C]verapamil; Antiarrhythmic agent; Blood brain barrier; Cerebral disorder; Central nervous system disease; Aralkylamine; Verapamil; Positron emission tomography; (R)-; Cerebrovascular disease; Emission tomography

We attempted to assess regional differences in cerebral P-glycoprotein (P-gp) function by performing paired positron emission tomography (PET) scans with the P-gp substrate (R)-[11C]verapamil in five healthy subjects before and after i.v. infusion of tariquidar (2 mg/kg). Comparison of tariquidar-in...