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000010453 0247_ $$2pmid$$apmid:20531460
000010453 0247_ $$2pmc$$apmc:PMC2949244
000010453 0247_ $$2DOI$$a10.1038/jcbfm.2010.65
000010453 0247_ $$2WOS$$aWOS:000280561900013
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000010453 041__ $$aeng
000010453 082__ $$a610
000010453 084__ $$2WoS$$aEndocrinology & Metabolism
000010453 084__ $$2WoS$$aHematology
000010453 084__ $$2WoS$$aNeurosciences
000010453 1001_ $$0P:(DE-Juel1)131679$$aElmenhorst, D.$$b0$$uFZJ
000010453 245__ $$aIn vivo and in vitro validation of reference tissue models for the mGluR5 ligand (11C)ABP688
000010453 260__ $$a[s.l.]$$bOvid$$c2010
000010453 300__ $$a1538 - 1549
000010453 3367_ $$0PUB:(DE-HGF)16$$2PUB:(DE-HGF)$$aJournal Article
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000010453 3367_ $$2DRIVER$$aarticle
000010453 440_0 $$03137$$aJournal of Cerebral Blood Flow and Metabolism$$v30$$x0271-678X
000010453 500__ $$aThis study was supported by the Alzheimer's Association new investigator grant, the Heinrich Hertz Foundation of the Ministry of Science and Technology, North-Rhine Westfalia, Germany (DE), Fonds de la Recherche en Sante du Quebec (FRSQ), Chercheur Burcier Award, Nussia and Andre Aisenstadt Foundation and Fondation Savoy.
000010453 520__ $$aThe primary objective of this study was to verify the suitability of reference tissue-based quantification methods of the metabotropic glutamate receptor type 5 (mGluR(5)) with [(11)C]ABP688. This study presents in vivo (Positron Emission Tomography (PET)) and in vitro (autoradiography) measurements of mGluR(5) densities in the same rats and evaluates both noninvasive and blood-dependent pharmacokinetic models for the quantification of [(11)C]ABP688 binding. Eleven rats underwent [(11)C]ABP688 PET scans. In five animals, baseline scans were compared with blockade experiments with the antagonist 1,2-methyl-6-(phenylethynyl)-pyridine (MPEP), and arterial blood samples were drawn and corrected for metabolites. Afterward, saturation-binding autoradiography was performed. Blocking with MPEP resulted in an average decrease of the total distribution volume (V(T)) between 43% and 58% (thalamus and caudate-putamen, respectively) but had no significant effect on cerebellar V(T) (mean reduction: -0.01%). Comparing binding potential (BP(ND)) based on the V(T) with noninvasively determined BP(ND) revealed an average negative bias of 0.7% in the caudate-putamen and an average positive bias of 3.1% in the low-binding regions. Scan duration of 50 minutes is required. The cerebellum is a suitable reference region for the quantification of mGluR(5) availability as measured with [(11)C]ABP688 PET in rats. Blood-based and reference region-based PET quantification shows a significant linear relationship to autoradiographic determinations.
000010453 536__ $$0G:(DE-Juel1)FUEK409$$2G:(DE-HGF)$$aFunktion und Dysfunktion des Nervensystems (FUEK409)$$cFUEK409$$x0
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000010453 650_2 $$2MeSH$$aAnimals
000010453 650_2 $$2MeSH$$aAutoradiography: methods
000010453 650_2 $$2MeSH$$aBinding Sites
000010453 650_2 $$2MeSH$$aBrain: metabolism
000010453 650_2 $$2MeSH$$aBrain: radionuclide imaging
000010453 650_2 $$2MeSH$$aCarbon Radioisotopes: analysis
000010453 650_2 $$2MeSH$$aCarbon Radioisotopes: metabolism
000010453 650_2 $$2MeSH$$aCarbon Radioisotopes: pharmacokinetics
000010453 650_2 $$2MeSH$$aKinetics
000010453 650_2 $$2MeSH$$aMale
000010453 650_2 $$2MeSH$$aOximes: analysis
000010453 650_2 $$2MeSH$$aOximes: metabolism
000010453 650_2 $$2MeSH$$aOximes: pharmacokinetics
000010453 650_2 $$2MeSH$$aPositron-Emission Tomography: methods
000010453 650_2 $$2MeSH$$aPyridines: analysis
000010453 650_2 $$2MeSH$$aPyridines: metabolism
000010453 650_2 $$2MeSH$$aPyridines: pharmacokinetics
000010453 650_2 $$2MeSH$$aRats
000010453 650_2 $$2MeSH$$aRats, Sprague-Dawley
000010453 650_2 $$2MeSH$$aReceptors, Metabotropic Glutamate: analysis
000010453 650_2 $$2MeSH$$aReceptors, Metabotropic Glutamate: metabolism
000010453 650_7 $$00$$2NLM Chemicals$$a3-(6-methylpyridin-2-ylethynyl)cyclohex-2-enone-O-methyloxime
000010453 650_7 $$00$$2NLM Chemicals$$aCarbon Radioisotopes
000010453 650_7 $$00$$2NLM Chemicals$$aOximes
000010453 650_7 $$00$$2NLM Chemicals$$aPyridines
000010453 650_7 $$00$$2NLM Chemicals$$aReceptors, Metabotropic Glutamate
000010453 650_7 $$00$$2NLM Chemicals$$ametabotropic glutamate receptor 5
000010453 650_7 $$2WoSType$$aJ
000010453 65320 $$2Author$$aautoradiography
000010453 65320 $$2Author$$ablocking
000010453 65320 $$2Author$$akinetic modeling
000010453 65320 $$2Author$$apositron emission tomography
000010453 65320 $$2Author$$a[C-11]ABP688
000010453 7001_ $$0P:(DE-HGF)0$$aMinuzzi, L.$$b1
000010453 7001_ $$0P:(DE-HGF)0$$aAliaga, A.$$b2
000010453 7001_ $$0P:(DE-HGF)0$$aRowley, J.$$b3
000010453 7001_ $$0P:(DE-HGF)0$$aMassarweh, G.$$b4
000010453 7001_ $$0P:(DE-HGF)0$$aDiksic, M.$$b5
000010453 7001_ $$0P:(DE-Juel1)131672$$aBauer, A.$$b6$$uFZJ
000010453 7001_ $$0P:(DE-HGF)0$$aRosa-Neto, P.$$b7
000010453 773__ $$0PERI:(DE-600)2039456-1$$a10.1038/jcbfm.2010.65$$gVol. 30, p. 1538 - 1549$$p1538 - 1549$$q30<1538 - 1549$$tJournal of cerebral blood flow & metabolism$$v30$$x0271-678X$$y2010
000010453 8567_ $$2Pubmed Central$$uhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC2949244
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000010453 9141_ $$y2010
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