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The adenosine triphosphate-binding cassette transporters P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) are 2 major gatekeepers at the blood-brain barrier (BBB) that restrict brain distribution of several clinically used drugs. In this study, we investigated the suitability of the radiolabeled Pgp/BCRP inhibitors (11)C-tariquidar and (11)C-elacridar to assess Pgp density in the human brain with PET.

the journal of nuclear medicine

Interaction of <sup>11</sup>C-Tariquidar and <sup>11</sup>C-Elacridar with P-Glycoprotein and Breast Cancer Resistance Protein at the Human Blood–Brain Barrier

Interaction of 11C-Tariquidar and 11C-Elacridar with P-Glycoprotein and Breast Cancer Resistance Protein at the Human Blood–Brain Barrier

Interaction of ¹¹C-Tariquidar and ¹¹C-Elacridar with P-Glycoprotein and Breast Cancer Resistance Protein at the Human Blood–Brain Barrier