TY  - JOUR
AU  - Kroll, Tina
AU  - Matusch, Andreas
AU  - Celik, A. Avdo
AU  - Wedekind, Franziska
AU  - Weißhaupt, Angela
AU  - Beer, Simone
AU  - Bauer, Andreas
TI  - [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
JO  - Nuclear medicine and biology
VL  - 41
IS  - 1
SN  - 1872-9614
CY  - Amsterdam [u.a.]
PB  - Elsevier Science
M1  - FZJ-2013-04138
SP  - 1-9
PY  - 2014
AB  - 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.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000328009300001
DO  - DOI:10.1016/j.nucmedbio.2013.09.001
UR  - https://juser.fz-juelich.de/record/137828
ER  -