Trial reportEuropean journal of nuclear medicine and molecular imaging2010
Biodistribution and dosimetry in humans of two inverse agonists to image cannabinoid CB1 receptors using positron emission tomography.
Trial report in European journal of nuclear medicine and molecular imaging, 2010. 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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The trial behind it
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Who cites it
12 citing papers in PubMed, 25 citations in OpenAlex.
- PET Molecular Imaging of the Endocannabinoid System in Psychiatric Disorders.Neuroscience bulletin · 2026Review
- Anti-stress neuropharmacological mechanisms and targets for addiction treatment: A translational framework.Neurobiology of stress · 2018Review
- Toxicity and radiation dosimetry studies of the serotonin transporter radioligand [(18) F]AFM in rats and monkeys.EJNMMI research · 2014Article
- Development of (18)F-labeled radiotracers for neuroreceptor imaging with positron emission tomography.Neuroscience bulletin · 2014Review
- Test-retest reproducibility of cannabinoid-receptor type 1 availability quantified with the PET ligand [¹¹C]MePPEP.NeuroImage · 2014Article
- 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
- Human biodistribution and dosimetry of 18F-JNJ42259152, a radioligand for phosphodiesterase 10A imaging.European journal of nuclear medicine and molecular imaging · 2013Article
- Binding of a tritiated inverse agonist to cannabinoid CB1 receptors is increased in patients with schizophrenia.Schizophrenia research · 2012Article
- Preclinical evaluation and quantification of [¹⁸F]MK-9470 as a radioligand for PET imaging of the type 1 cannabinoid receptor in rat brain.European journal of nuclear medicine and molecular imaging · 2012Article
- Suggested pathway to assess radiation safety of 11C-labeled PET tracers for first-in-human studies.European journal of nuclear medicine and molecular imaging · 2012Article
- [¹²⁵I]SD-7015 reveals fine modalities of CB₁ cannabinoid receptor density in the prefrontal cortex during progression of Alzheimer's disease.Neurochemistry international · 2012Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
Abstract
purposeCannabinoid subtype 1 (CB(1)) receptors are found in nearly every organ in the body, may be involved in several neuropsychiatric and metabolic disorders, and are therefore an active target for pharmacotherapy and biomarker development. We recently reported brain imaging of CB(1) receptors with two PET radioligands: (11)C-MePPEP and (18)F-FMPEP-d (2). Here we describe the biodistribution and dosimetry estimates for these two radioligands.
methodsSeven healthy subjects (four men and three women) underwent whole-body PET scans for 120 min after injection with (11)C-MePPEP. Another seven healthy subjects (two men and five women) underwent whole-body PET scans for 300 min after injection with (18)F-FMPEP-d (2). Residence times were acquired from regions of interest drawn on tomographic images of visually identifiable organs for both radioligands and from radioactivity excreted in urine for (18)F-FMPEP-d (2).
resultsThe effective doses of (11)C-MePPEP and (18)F-FMPEP-d (2) are 4.6 and 19.7 microSv/MBq, respectively. Both radioligands demonstrated high uptake of radioactivity in liver, lung, and brain shortly after injection and accumulated radioactivity in bone marrow towards the end of the scan. After injection of (11)C-MePPEP, radioactivity apparently underwent hepatobiliary excretion only, while radioactivity from (18)F-FMPEP-d (2) showed both hepatobiliary and urinary excretion.
conclusion(11)C-MePPEP and (18)F-FMPEP-d (2) yield an effective dose similar to other PET radioligands labeled with either (11)C or (18)F. The high uptake in brain confirms the utility of these two radioligands to image CB(1) receptors in brain, and both may also be useful to image CB(1) receptors in the periphery.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.