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| 024 | 7 | _ | |a 0161-5505 |2 ISSN |
| 024 | 7 | _ | |a 1535-5667 |2 ISSN |
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| 037 | _ | _ | |a FZJ-2013-02757 |
| 041 | _ | _ | |a ENG |
| 082 | _ | _ | |a 610 |
| 100 | 1 | _ | |a Elmenhorst, David |0 P:(DE-Juel1)131679 |b 0 |u fzj |e Corresponding author |
| 245 | _ | _ | |a In Vivo Kinetic and Steady-State Quantification of 18F-CPFPX Binding to Rat Cerebral A1 Adenosine Receptors: Validation by Displacement and Autoradiographic Experiments |
| 260 | _ | _ | |a Reston, Va. |c 2013 |b SNM84042 |
| 264 | _ | 1 | |3 online |2 Crossref |b Society of Nuclear Medicine |c 2013-06-05 |
| 264 | _ | 1 | |3 print |2 Crossref |b Society of Nuclear Medicine |c 2013-08-01 |
| 264 | _ | 1 | |3 print |2 Crossref |b Society of Nuclear Medicine |c 2013-08-01 |
| 336 | 7 | _ | |a Journal Article |b journal |m journal |0 PUB:(DE-HGF)16 |s 1378707509_1314 |2 PUB:(DE-HGF) |
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| 336 | 7 | _ | |a article |2 DRIVER |
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| 520 | _ | _ | |a In vivo imaging of the A1 adenosine receptor (A1AR) using (18)F-8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ((18)F-CPFPX) and PET has become an important tool for studying physiologic and pathologic states of the human brain. However, dedicated experimental settings for small-animal studies are still lacking. The aim of the present study was therefore to develop and evaluate suitable pharmacokinetic models for the quantification of the cerebral A1AR in high-resolution PET. METHODS: On a dedicated animal PET scanner, 15 rats underwent (18)F-CPFPX PET scans of 120-min duration. In all animals, arterial blood samples were drawn and corrected for metabolites. The radioligand was injected either as a bolus or as a bolus plus constant infusion. For the definition of unspecific binding, the A1AR selective antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) was applied. After PET, the brains of 9 animals were dissected and in vitro saturation binding was performed using high-resolution (3)H-DPCPX autoradiography. RESULTS: The kinetics of (18)F-CPFPX were well described by either compartmental or noncompartmental models based on arterial input function. The resulting distribution volume ratio correlated with a low bias toward identity with the binding potential derived from a reference region (olfactory bulb) approach. Furthermore, PET quantification correlated significantly with autoradiographic in vitro data. Blockade of the A1AR with DPCPX identified specific binding of about 45% in the reference region olfactory bulb. CONCLUSION: The present study provides evidence that (18)F-CPFPX PET based on a reference tissue approach can be performed quantitatively in rodents in selected applications. Specific binding in the reference region needs careful consideration for quantitative investigations. |
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| 700 | 1 | _ | |a Kroll, Tina |0 P:(DE-Juel1)131691 |b 1 |u fzj |
| 700 | 1 | _ | |a Wedekind, Franziska |0 P:(DE-Juel1)131711 |b 2 |
| 700 | 1 | _ | |a Weißhaupt, Angela |0 P:(DE-Juel1)131712 |b 3 |
| 700 | 1 | _ | |a Beer, Simone |0 P:(DE-Juel1)133864 |b 4 |u fzj |
| 700 | 1 | _ | |a Bauer, Andreas |0 P:(DE-Juel1)131672 |b 5 |u fzj |
| 773 | 1 | 8 | |a 10.2967/jnumed.112.115576 |b : Society of Nuclear Medicine, 2013-06-05 |n 8 |p 1411-1419 |3 journal-article |2 Crossref |t Journal of Nuclear Medicine |v 54 |y 2013 |x 0161-5505 |
| 773 | _ | _ | |a 10.2967/jnumed.112.115576 |g p. jnumed.112.115576 |p 1411-1419 |n 8 |0 PERI:(DE-600)2040222-3 |t Journal of nuclear medicine |v 54 |y 2013 |x 0161-5505 |
| 856 | 4 | _ | |u http://www.ncbi.nlm.nih.gov/pubmed/?term=PMID%3A+23740103 |
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