ArticleEuropean journal of nuclear medicine and molecular imaging2012
Preclinical evaluation and quantification of [¹⁸F]MK-9470 as a radioligand for PET imaging of the type 1 cannabinoid receptor in rat brain.
Article in European journal of nuclear medicine and molecular imaging, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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12 citing papers in PubMed.
- Progress on the application of positron emission tomography imaging of cannabinoid type 1 receptor in neuropsychiatric diseases.Zhejiang da xue xue bao. Yi xue ban = Journal of Zhejiang University. Medical sciences · 2021Review
- Ruthenium-MediatedACS chemical neuroscience · 2020Article
- Quantification of the Cannabinoid Type 1 Receptor Availability in the Mouse Brain.Frontiers in neuroanatomy · 2020Article
- Is There a Role for GPCR Agonist Radiotracers in PET Neuroimaging?Frontiers in molecular neuroscience · 2019Review
- Sifting through the surfeit of neuroinflammation tracers.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2018Review
- Changes in cerebral CB1 receptor availability after acute and chronic alcohol abuse and monitored abstinence.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
- Small animal PET imaging of the type 1 cannabinoid receptor in a rodent model for anorexia nervosa.European journal of nuclear medicine and molecular imaging · 2014Article
- Transient changes in the endocannabinoid system after acute and chronic ethanol exposure and abstinence in the rat: a combined PET and microdialysis study.European journal of nuclear medicine and molecular imaging · 2013Article
- Evaluation of cannabinoid type 1 receptor expression in the rat brain using [¹⁸F]MK-9470 microPET.European journal of nuclear medicine and molecular imaging · 2013Article
- 18F-MK-9470 PET imaging of the type 1 cannabinoid receptor in prostate carcinoma: a pilot study.EJNMMI research · 2013Article
- In vivo SPECT and ex vivo autoradiographic brain imaging of the novel selective CB1 receptor antagonist radioligand [125I]SD7015 in CB1 knock-out and wildtype mouse.Brain research bulletin · 2013Article
- Small-animal PET imaging of the type 1 and type 2 cannabinoid receptors in a photothrombotic stroke model.European journal of nuclear medicine and molecular imaging · 2012Article
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5 authors.
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Abstract
purpose[(18)F]MK-9470 is an inverse agonist for the type 1 cannabinoid (CB1) receptor allowing its use in PET imaging. We characterized the kinetics of [(18)F]MK-9470 and evaluated its ability to quantify CB1 receptor availability in the rat brain.
methodsDynamic small-animal PET scans with [(18)F]MK-9470 were performed in Wistar rats on a FOCUS-220 system for up to 10 h. Both plasma and perfused brain homogenates were analysed using HPLC to quantify radiometabolites. Displacement and blocking experiments were done using cold MK-9470 and another inverse agonist, SR141716A. The distribution volume (V(T)) of [(18)F]MK-9470 was used as a quantitative measure and compared to the use of brain uptake, expressed as SUV, a simplified method of quantification.
resultsThe percentage of intact [(18)F]MK-9470 in arterial plasma samples was 80 ± 23 % at 10 min, 38 ± 30 % at 40 min and 13 ± 14 % at 210 min. A polar radiometabolite fraction was detected in plasma and brain tissue. The brain radiometabolite concentration was uniform across the whole brain. Displacement and pretreatment studies showed that 56 % of the tracer binding was specific and reversible. V (T) values obtained with a one-tissue compartment model plus constrained radiometabolite input had good identifiability (≤10 %). Ignoring the radiometabolite contribution using a one-tissue compartment model alone, i.e. without constrained radiometabolite input, overestimated the [(18)F]MK-9470 V(T), but was correlated. A correlation between [(18)F]MK-9470 V(T) and SUV in the brain was also found (R(2) = 0.26-0.33; p ≤ 0.03).
conclusionWhile the presence of a brain-penetrating radiometabolite fraction complicates the quantification of [(18)F]MK-9470 in the rat brain, its tracer kinetics can be modelled using a one-tissue compartment model with and without constrained radiometabolite input.
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