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| 001 | 824539 | ||
| 005 | 20220930130111.0 | ||
| 024 | 7 | _ | |a 10.1016/j.nucmedbio.2016.09.004 |2 doi |
| 024 | 7 | _ | |a 0969-8051 |2 ISSN |
| 024 | 7 | _ | |a 1872-9614 |2 ISSN |
| 024 | 7 | _ | |a WOS:000390836100006 |2 WOS |
| 037 | _ | _ | |a FZJ-2016-07111 |
| 082 | _ | _ | |a 610 |
| 100 | 1 | _ | |a Kreft, Sabrina |0 P:(DE-Juel1)144437 |b 0 |
| 245 | _ | _ | |a New potent A1 adenosine receptor radioligands for positron emission tomography |
| 260 | _ | _ | |a Amsterdam [u.a.] |c 2017 |b Elsevier Science |
| 336 | 7 | _ | |a article |2 DRIVER |
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| 520 | _ | _ | |a 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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| 700 | 1 | _ | |a Bier, Dirk |0 P:(DE-Juel1)131810 |b 1 |e Corresponding author |
| 700 | 1 | _ | |a Holschbach, Marcus |0 P:(DE-Juel1)131824 |b 2 |
| 700 | 1 | _ | |a Schulze, Annette |0 P:(DE-Juel1)131847 |b 3 |
| 700 | 1 | _ | |a Coenen, Heinrich Hubert |0 P:(DE-Juel1)131816 |b 4 |
| 773 | _ | _ | |a 10.1016/j.nucmedbio.2016.09.004 |g Vol. 44, p. 69 - 77 |0 PERI:(DE-600)1498538-x |p 69 - 77 |t Nuclear medicine and biology |v 44 |y 2017 |x 0969-8051 |
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