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024 7 _ |a 10.1016/j.nucmedbio.2013.09.001
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037 _ _ |a FZJ-2013-04138
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100 1 _ |a Kroll, Tina
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245 _ _ |a [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
260 _ _ |a Amsterdam [u.a.]
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520 _ _ |a 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.
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700 1 _ |a Matusch, Andreas
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700 1 _ |a Celik, A. Avdo
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700 1 _ |a Wedekind, Franziska
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700 1 _ |a Weißhaupt, Angela
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700 1 _ |a Beer, Simone
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700 1 _ |a Bauer, Andreas
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773 _ _ |a 10.1016/j.nucmedbio.2013.09.001
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