This title appears in the Scientific Report :
2017
Please use the identifier:
http://dx.doi.org/10.1016/j.nucmedbio.2016.09.004 in citations.
New potent A1 adenosine receptor radioligands for positron emission tomography
New potent A1 adenosine receptor radioligands for positron emission tomography
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 n...
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Personal Name(s): | Kreft, Sabrina |
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Bier, Dirk (Corresponding author) / Holschbach, Marcus / Schulze, Annette / Coenen, Heinrich Hubert | |
Contributing Institute: |
Nuklearchemie; INM-5 |
Published in: | Nuclear medicine and biology, 44 (2017) S. 69 - 77 |
Imprint: |
Amsterdam [u.a.]
Elsevier Science
2017
|
DOI: |
10.1016/j.nucmedbio.2016.09.004 |
Document Type: |
Journal Article |
Research Program: |
Neuroimaging |
Publikationsportal JuSER |
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. |