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Imaging of Cyclosporine Inhibition of P-Glycoprotein Activity Using 11C-Verapamil in the Brain: Studies of Healthy Humans
The Journal of Nuclear Medicine, 07/21/09
Muzi M et al. – 11C–verapamil and compartmental analysis can estimate P–gp activity at the BBB by imaging before and during P–gp inhibition by CsA, indicated by a change in verapamil transport. Inhibition of P–gp unmasks verapamil trapping in brain tissue that requires a 2C model for long imaging times; however, transport can be effectively measured using a short scan time with a 1C10 model, avoiding complications with labeled metabolites and tracer retention.
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