| Kinetic analysis of the cannabinoid-1 receptor PET tracer [(18)F]MK-9470 in human brain. | |
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MedLine Citation:
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PMID: 20033684 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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PURPOSE: Quantitative imaging of the type 1 cannabinoid receptor (CB1R) opens perspectives for many neurological and psychiatric disorders. We characterized the kinetics and reproducibility of the CB1R tracer [(18)F]MK-9470 in human brain. METHODS: [(18)F]MK-9470 data were analysed using reversible models and the distribution volume V (T) and V (ND) k (3) (V (ND) k (3) = K (1) k (2)) were estimated. Tracer binding was also evaluated using irreversible kinetics and the irreversible uptake constant K (i) and fractional uptake rate (FUR) were estimated. The effect of blood flow on these parameters was evaluated. Additionally, the possibility of determining the tracer plasma kinetics using a reduced number of blood samples was also examined. RESULTS: A reversible two-tissue compartment model using a global k (4) value was necessary to describe brain kinetics. Both V (T) and V (ND) k (3) were estimated satisfactorily and their test-retest variability was between 10% and 30%. Irreversible methods adequately described brain kinetics and FUR values were equivalent to K (i). The linear relationship between K (i) and V (ND) k (3) demonstrated that K (i) or FUR and thus the simple measure of tracer brain uptake provide CB1R availability information. The test-retest variability of K (i) and FUR was <10% and estimates were independent of blood flow. Brain uptake can be used as a receptor availability index, albeit at the expense of potential bias due to between-subject differences in tracer plasma kinetics. CONCLUSION: [(18)F]MK-9470 specific binding can be accurately determined using FUR values requiring a short scan 90 to 120 min after tracer administration. Our results suggest that [(18)F]MK-9470 plasma kinetics can be assessed using a few venous samples. |
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Authors:
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Sandra Marina Sanabria-Bohórquez; Terence G Hamill; Karolien Goffin; Inge De Lepeleire; Guy Bormans; H Donald Burns; Koen Van Laere |
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Publication Detail:
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Type: Clinical Trial; Journal Article Date: 2009-12-24 |
Journal Detail:
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Title: European journal of nuclear medicine and molecular imaging Volume: 37 ISSN: 1619-7089 ISO Abbreviation: Eur. J. Nucl. Med. Mol. Imaging Publication Date: 2010 May |
Date Detail:
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Created Date: 2010-04-14 Completed Date: 2010-07-07 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101140988 Medline TA: Eur J Nucl Med Mol Imaging Country: Germany |
Other Details:
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Languages: eng Pagination: 920-33 Citation Subset: IM |
Affiliation:
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Imaging, Merck Research Laboratories, Sumneytown Pike WP44D-2, West Point, PA 19486, USA. sandra_sanabria@merck.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Adult Brain / metabolism* Cerebrovascular Circulation Feasibility Studies Female Humans Kinetics Male Middle Aged Models, Biological Positron-Emission Tomography* Pyridines / blood, diagnostic use, metabolism*, pharmacokinetics* Radioactive Tracers Receptor, Cannabinoid, CB1 / metabolism* Young Adult |
| Chemical | |
Reg. No./Substance:
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0/MK-9470; 0/Pyridines; 0/Radioactive Tracers; 0/Receptor, Cannabinoid, CB1 |
| Comments/Corrections | |
Comment In:
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Eur J Nucl Med Mol Imaging. 2010 May;37(5):917-9
[PMID:
20358196
]
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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