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@ARTICLE{Kreft:824539,
author = {Kreft, Sabrina and Bier, Dirk and Holschbach, Marcus and
Schulze, Annette and Coenen, Heinrich Hubert},
title = {{N}ew potent {A}1 adenosine receptor radioligands for
positron emission tomography},
journal = {Nuclear medicine and biology},
volume = {44},
issn = {0969-8051},
address = {Amsterdam [u.a.]},
publisher = {Elsevier Science},
reportid = {FZJ-2016-07111},
pages = {69 - 77},
year = {2017},
abstract = {8-Cyclopentyl-3-(3-[18F]fluoropropyl)-1-propylxanthine
([18F]CPFPX) is meanwhile an accepted receptor ligand to
examine the A1 adenosine receptor (A1AR) in humans by
positron emission tomography (PET). A major drawback of this
compound is its rather fast metabolic degradation in
vivo.Therefore two new xanthine derivatives, namely
8-cyclobutyl-1-cyclopropymethyl-3-(3-fluoropropyl)xanthine
(CBCPM; 5) and
1-cyclopropylmethyl-3-(3-fluoropropyl)-8-(1-methylcyclobutyl)xanthine
(CPMMCB; 6) were designed and synthesized as potential
alternatives to CPFPX. In membrane binding studies both
compounds showed nanomolar affinity for the A1AR. In vitro
autoradiographic studies of [18F]5 and [18F]6, using rat
brain slices, showed the expected accumulation in regions
known to have a high adenosine A1 receptor expression while
exhibiting the necessary low unspecific binding. However, in
vitro metabolite studies using human liver microsomes
revealed a comparable metabolic degradation rate for both
new xanthine derivatives and CPFPX.},
cin = {INM-5},
ddc = {610},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {573 - Neuroimaging (POF3-573)},
pid = {G:(DE-HGF)POF3-573},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000390836100006},
doi = {10.1016/j.nucmedbio.2016.09.004},
url = {https://juser.fz-juelich.de/record/824539},
}