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Society of Nuclear Medicine, Journal of Nuclear Medicine, 8(50), p. 1267-1275, 2009

DOI: 10.2967/jnumed.108.059162

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Imaging of Cyclosporine Inhibition of P-Glycoprotein Activity Using 11C-Verapamil in the Brain: Studies of Healthy Humans

Journal article published in 2009 by Mark Muzi, David A. Mankoff, Jeanne M. Link, Steve Shoner, Ann C. Collier, Lucy Sasongko, Jashvant D. Unadkat ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

The multiple-drug resistance (MDR) transporter P-glycoprotein (P-gp) is highly expressed at the human blood–brain barrier (BBB). P-gp actively effluxes a wide variety of drugs from the central nervous system, including anticancer drugs. We have previously demonstrated P-gp activity at the human BBB using PET of 11C-verapamil distribution into the brain in the absence and presence of the P-gp inhibitor cyclosporine-A (CsA). Here we extend the initial noncompartmental analysis of these data and apply compartmental modeling to these human verapamil imaging studies.