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Intravenous infusion for the controlled exposure to the dual ABCB1 and ABCG2 inhibitor elacridar in nonhuman primates

Archive ouverte | Goutal, Sebastien | CCSD

International audience. Elacridar (GF120918) is a highly potent inhibitor of both P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2), the main efflux transporters expressed at the blood-brain barrie...

Diphenhydramine as a selective probe to study H + -antiporter function at the blood–brain barrier: Application to [ 11 C]diphenhydramine positron emission tomography imaging

Archive ouverte | Auvity, Sylvain | CCSD

International audience. Diphenhydramine, a sedative histamine H 1 -receptor (H 1 R) antagonist, was evaluated as a probe to measure drug/H + -antiporter function at the blood–brain barrier. In situ brain perfusion e...

Automated two-step manufacturing of [11C]glyburide radiopharmaceutical for PET imaging in humans

Archive ouverte | Caillé, Fabien | CCSD

International audience. Introduction: Glyburide is an approved anti-diabetes drug binding to the sulfonylurea receptors-1 (SUR-1) and substrate of solute carrier (SLC) transporters, which can be isotopically radiola...

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