The impact of the BBB on the pharmacokinetics of drugs: Investigations by PET

Jashvant D. Unadkat, Ban Ke, Sara Eyal

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

1 Scopus citations


The blood brain barrier (BBB) impedes many neuropharmaceuticals from eliciting their desirable pharmacological or toxicological effect. A crucial component of this barrier is the ATP-driven drug efflux pump P-glycoprotein, which prevents the entry of xenobiotics into the brain. P-gp’s activity is also implicated in pathologies such as neurodegenerative disorders and refractory brain diseases. PET allows non-invasive in vivo assessment of P-gp’s impact on drug disposition in the CNS. Recently, a number of P-gp ligands have been synthesized for PET studies. Using the most-established P-gp ligand [11C]-verapamil, as an example, methods to quantify P-gp activity at the BBB are discussed and compared. Drug-drug interaction (DDI) studies in the CNS following modulation of P-gp activity are also presented. Finally, the application of PET methodology to study P-gp function in the diseased brain is discussed.

Original languageAmerican English
Title of host publicationTrends on the Role of PET in Drug Development
PublisherWorld Scientific Publishing Co.
Number of pages40
ISBN (Electronic)9789814317740
ISBN (Print)981431773X, 9789814317733
StatePublished - 1 Jan 2012

Bibliographical note

Publisher Copyright:
© 2012 World Scientific Publishing Co. Pte. Ltd. All rights reserved.


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