2008
DOI: 10.1016/j.neuroimage.2008.03.004
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Positron emission tomography imaging using an inverse agonist radioligand to assess cannabinoid CB1 receptors in rodents

Abstract: Abstract[ 11 C]MePPEP is an inverse agonist and a radioligand developed to image cannabinoid CB 1 receptors with positron emission tomography (PET). It provides reversible, high specific signal in monkey brain. We assessed [ 11 C]MePPEP in rodent brain with regard to receptor selectivity, susceptibility to transport by P-glycoprotein (P-gp), sensitivity to displacement by agonists, and accumulation of radiometabolites. We used CB 1 receptor knockout mice and P-gp knockout mice to assess receptor selectivity an… Show more

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Cited by 45 publications
(35 citation statements)
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“…To evaluate the effect of the possible accumulation of radiometabolites on the estimation of V T , we performed a time-stability analysis of V T . The increase in V T with an increase in scan length could be interpreted as evidence for the accumulation of radiometabolites in the brain (30). In the current study, V T values by the 2-TCM in the putamen and cerebellum with 60-min data were approximately 94% and 90% of terminal values with 90-min data (Fig.…”
Section: Figuresupporting
confidence: 59%
“…To evaluate the effect of the possible accumulation of radiometabolites on the estimation of V T , we performed a time-stability analysis of V T . The increase in V T with an increase in scan length could be interpreted as evidence for the accumulation of radiometabolites in the brain (30). In the current study, V T values by the 2-TCM in the putamen and cerebellum with 60-min data were approximately 94% and 90% of terminal values with 90-min data (Fig.…”
Section: Figuresupporting
confidence: 59%
“…Most of the compounds to date produce small specific signals due to high lipophilicity and/or low affinity for CB1R, with the exception of [ 11 C] JHU75528 [3,4], [ 11 C]MePPEP [5,6], and [ 18 F]MK-9470 [7]. Applying the criteria of high affinity and selectivity for CB1R, appropriate lipophilicity for a CB1R radiotracer and synthesis via reliable radiochemistry suitable to a clinical setting, we labeled and carried out rhesus PET imaging studies with a number of potential CB1R PET tracers [9].…”
Section: Discussionmentioning
confidence: 99%
“…In addition to studying cannabinoid system biology, a CB1R SPECT or PET tracer could be used as a biomarker for target engagement to measure receptor occupancy of CB1R therapeutic compounds in preclinical as well as clinical studies and to guide dose selection in clinical trials. Recently, notable progress has been made in this area with the disclosure of [ 11 C] JHU75528 [3,4], [ 11 C]MePPEP [5,6], and [ 18 F]MK-9470 [7,8] (Fig. 1).…”
Section: Introductionmentioning
confidence: 99%
“…is that the tracer binds to the entire opioidergic system, thus providing a rather composite view of opioidergic neurotransmission evoked by exercise challenges. As the endocannabinoid system is also of great interest in the context of exercise research (Dietrich and McDaniel 2004 ;Sparling et al 2003 ) , future applications are awaited using novel compounds that label endocannabinoid receptors (Evens et al 2009 ;Terry et al 2008 ;Van Laere et al 2008 ) . For a detailed summary of the available opioidergic tracers, we refer to a recent review article from our group (Boecker et al 2008a ) .…”
Section: Opioid Receptor Petmentioning
confidence: 99%