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@ARTICLE{Kroll:137828,
author = {Kroll, Tina and Matusch, Andreas and Celik, A. Avdo and
Wedekind, Franziska and Weißhaupt, Angela and Beer, Simone
and Bauer, Andreas},
title = {[18{F}]{A}ltanserin and small animal {PET}: {I}mpact of
multidrug efflux transporters on ligand brain uptake and
subsequent quantification of 5-{HT}2{A} receptor densities
in the rat brain},
journal = {Nuclear medicine and biology},
volume = {41},
number = {1},
issn = {1872-9614},
address = {Amsterdam [u.a.]},
publisher = {Elsevier Science},
reportid = {FZJ-2013-04138},
pages = {1-9},
year = {2014},
abstract = {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.},
cin = {INM-2 / INM-4},
ddc = {610},
cid = {I:(DE-Juel1)INM-2-20090406 / I:(DE-Juel1)INM-4-20090406},
pnm = {333 - Pathophysiological Mechanisms of Neurological and
Psychiatric Diseases (POF2-333)},
pid = {G:(DE-HGF)POF2-333},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000328009300001},
doi = {10.1016/j.nucmedbio.2013.09.001},
url = {https://juser.fz-juelich.de/record/137828},
}