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@ARTICLE{Elmenhorst:10453,
author = {Elmenhorst, D. and Minuzzi, L. and Aliaga, A. and Rowley,
J. and Massarweh, G. and Diksic, M. and Bauer, A. and
Rosa-Neto, P.},
title = {{I}n vivo and in vitro validation of reference tissue
models for the m{G}lu{R}5 ligand (11{C}){ABP}688},
journal = {Journal of cerebral blood flow $\&$ metabolism},
volume = {30},
issn = {0271-678X},
address = {[s.l.]},
publisher = {Ovid},
reportid = {PreJuSER-10453},
pages = {1538 - 1549},
year = {2010},
note = {This 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.},
abstract = {The 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.},
keywords = {Animals / Autoradiography: methods / Binding Sites / Brain:
metabolism / Brain: radionuclide imaging / Carbon
Radioisotopes: analysis / Carbon Radioisotopes: metabolism /
Carbon Radioisotopes: pharmacokinetics / Kinetics / Male /
Oximes: analysis / Oximes: metabolism / Oximes:
pharmacokinetics / Positron-Emission Tomography: methods /
Pyridines: analysis / Pyridines: metabolism / Pyridines:
pharmacokinetics / Rats / Rats, Sprague-Dawley / Receptors,
Metabotropic Glutamate: analysis / Receptors, Metabotropic
Glutamate: metabolism /
3-(6-methylpyridin-2-ylethynyl)cyclohex-2-enone-O-methyloxime
(NLM Chemicals) / Carbon Radioisotopes (NLM Chemicals) /
Oximes (NLM Chemicals) / Pyridines (NLM Chemicals) /
Receptors, Metabotropic Glutamate (NLM Chemicals) /
metabotropic glutamate receptor 5 (NLM Chemicals) / J
(WoSType)},
cin = {INM-2},
ddc = {610},
cid = {I:(DE-Juel1)INM-2-20090406},
pnm = {Funktion und Dysfunktion des Nervensystems (FUEK409) /
89574 - Theory, modelling and simulation (POF2-89574)},
pid = {G:(DE-Juel1)FUEK409 / G:(DE-HGF)POF2-89574},
shelfmark = {Endocrinology $\&$ Metabolism / Hematology / Neurosciences},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:20531460},
pmc = {pmc:PMC2949244},
UT = {WOS:000280561900013},
doi = {10.1038/jcbfm.2010.65},
url = {https://juser.fz-juelich.de/record/10453},
}