%0 Journal Article
%A Kroll, Tina
%A Matusch, Andreas
%A Celik, A. Avdo
%A Wedekind, Franziska
%A Weißhaupt, Angela
%A Beer, Simone
%A Bauer, Andreas
%T [18F]Altanserin and small animal PET: Impact of multidrug efflux transporters on ligand brain uptake and subsequent quantification of 5-HT2A receptor densities in the rat brain
%J Nuclear medicine and biology
%V 41
%N 1
%@ 1872-9614
%C Amsterdam [u.a.]
%I Elsevier Science
%M FZJ-2013-04138
%P 1-9
%D 2014
%X The selective 5-hydroxytryptamine type 2a receptor (5-HT2AR) radiotracer [18F]altanserin is a promising ligand for in vivo brain imaging in rodents. However, [18F]altanserin is a substrate of P-glycoprotein (P-gp) in rats. Its applicability might therefore be constrained by both a differential expression of P-gp under pathological conditions, e.g. epilepsy, and its relatively low cerebral uptake. The aim of the present study was therefore twofold: (i) to investigate whether inhibition of multidrug transporters (MDT) is suitable to enhance the cerebral uptake of [18F]altanserin in vivo and (ii) to test different pharmacokinetic, particularly reference tissue-based models for exact quantification of 5-HT2AR densities in the rat brain.
%F PUB:(DE-HGF)16
%9 Journal Article
%U <Go to ISI:>//WOS:000328009300001
%R 10.1016/j.nucmedbio.2013.09.001
%U https://juser.fz-juelich.de/record/137828