ArticleMolecular imaging and biology2013
Preclinical safety assessment of the 5-HT2A receptor agonist PET radioligand [ 11C]Cimbi-36.
Article in Molecular imaging and biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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Who cites it
25 citing papers in PubMed.
- Serotonin 2A receptor agonist binding in the human brain with [¹¹C]Cimbi-36.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2014Trial
- Psilocybin as Transformative Fast-Acting Antidepressant: Pharmacological Properties and Molecular Mechanisms.Fundamental & clinical pharmacology · 2025Review
- Neuroimaging and the Investigation of Drug-Drug Interactions Involving Psychedelics.Neuroscience insights · 2024Article
- Neuroimaging in psychedelic drug development: past, present, and future.Molecular psychiatry · 2023Review
- AnFrontiers in neuroscience · 2022Article
- 25CN-NBOMe Metabolites in Rat Urine, Human Liver Microsomes andMetabolites · 2021Article
- A Single Dose of Psilocybin Increases Synaptic Density and Decreases 5-HTInternational journal of molecular sciences · 2021Article
- DARK Classics in Chemical Neuroscience: NBOMes.ACS chemical neuroscience · 2020Review
- Human biodistribution and radiation dosimetry of the 5-HTEJNMMI research · 2019Article
- Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging.Medicinal research reviews · 2019Review
- In vivo PET Imaging of [11C]CIMBI-5, a 5-HT2AR Agonist Radiotracer in Nonhuman Primates.Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques · 2019Article
- From simultaneous to synergistic MR-PET brain imaging: A review of hybrid MR-PET imaging methodologies.Human brain mapping · 2018Review
- Effect of Hallucinogens on Unconditioned Behavior.Current topics in behavioral neurosciences · 2018Review
- Pharmacology and Toxicology of N-Benzylphenethylamine ("NBOMe") Hallucinogens.Current topics in behavioral neurosciences · 2017Review
- In vivo evaluation of [Bioorganic & medicinal chemistry letters · 2017Article
- Synthesis and in vitro evaluation of [18F]FECIMBI-36: A potential agonist PET ligand for 5-HT2A/2C receptors.Bioorganic & medicinal chemistry letters · 2015Article
- Recent advances in the neuropsychopharmacology of serotonergic hallucinogens.Behavioural brain research · 2015Review
- Correlating the metabolic stability of psychedelic 5-HT₂A agonists with anecdotal reports of human oral bioavailability.Neurochemical research · 2014Article
- High-performance liquid chromatography with tandem mass spectrometry for the determination of nine hallucinogenic 25-NBOMe designer drugs in urine specimens.Journal of analytical toxicology · 2014Article
- Synthesis and structure-activity relationships of N-benzyl phenethylamines as 5-HT2A/2C agonists.ACS chemical neuroscience · 2014Article
Corrections and comments
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Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purpose[11C]Cimbi-36 was recently developed as an agonist radioligand for brain imaging of serotonin 2A receptors (5-HT2A) with positron emission tomography (PET). This may be used to quantify the high-affinity state of 5-HT2A receptors and may have the potential to quantify changes in cerebral 5-HT levels in vivo. We here investigated safety aspects related to clinical use of [11C]Cimbi-36, including radiation dosimetry and in vivo pharmacology. PROCEDURES: [11C]Cimbi-36 was injected in rats or pigs, and radiation dosimetry was examined by ex vivo dissection or with PET scanning, respectively. Based on animal data, the Organ Level INternal Dose Assessment software was used to estimate extrapolated human dosimetry for [11C]Cimbi-36. The 5-HT2A receptor agonist actions of [11C]Cimbi-36 in vivo pharmacological effects in mice elicited by increasing doses of Cimbi-36 were assessed with the head-twitch response (HTR).
resultsThe effective dose as extrapolated from both rat and pig data was low, 7.67 and 4.88 μSv/MBq, respectively. In addition, the estimated absorbed radiation dose to human target organs did not exceed safety levels. Administration of 0.5 mg/kg Cimbi-36 leads to significant HTR compared to saline, whereas 0.05 mg/kg Cimbi-36 (doses much larger than those given in conjunction with a PET scan) did not elicit a significant HTR.
conclusionsAdministration of tracer doses of [11C]Cimbi-36 does not seem to be associated with unusual radiation burden or adverse clinical effects.
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