Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood− brain …

…, C Kuntner, JP Bankstahl, M Bankstahl…

Index: Doerner, Bernd; Kuntner, Claudia; Bankstahl, Jens P.; Bankstahl, Marion; Stanek, Johann; Wanek, Thomas; Stundner, Gloria; Mairinger, Severin; Loescher, Wolfgang; Mueller, Markus; Langer, Oliver; Erker, Thomas Journal of Medicinal Chemistry, 2009 , vol. 52, # 19 p. 6073 - 6082

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Citation Number: 56

Abstract

With the aim to develop a positron emission tomography (PET) tracer to assess the distribution of P-glycoprotein (P-gp) at the blood− brain barrier (BBB) in vivo, the potent third- generation P-gp inhibitor elacridar (1) was labeled with 11C by reaction of O-desmethyl 1 with [11C]-methyl triflate. In vitro autoradiography and small-animal PET imaging of [11C]-1 was performed in rats (n= 3), before and after administration of unlabeled 1, as well as in ...