Journal Article

FZJ-2016-07111

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png New potent A1 adenosine receptor radioligands for positron emission tomography

Kreft, S.FZJ* ; Bier, D. (Corresponding author)FZJ* ; Holschbach, M.FZJ* ; Schulze, A.FZJ* ; Coenen, H. H.FZJ*

2017
Elsevier Science Amsterdam [u.a.]

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Please use a persistent id in citations: doi:10.1016/j.nucmedbio.2016.09.004

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.

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Contributing Institute(s):

1. Nuklearchemie (INM-5)

Research Program(s):

1. 573 - Neuroimaging (POF3-573) (POF3-573)

Appears in the scientific report 2017

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