Preclinical Safety Assessment of the 5-HT2A Receptor Agonist PET Radioligand [11C]Cimbi-36
@article{Ettrup2012PreclinicalSA, title={Preclinical Safety Assessment of the 5-HT2A Receptor Agonist PET Radioligand [11C]Cimbi-36}, author={A. Ettrup and S. Holm and M. Hansen and M. Wasim and M. A. Santini and M. Palner and J. Madsen and C. Svarer and J. Kristensen and G. Knudsen}, journal={Molecular Imaging and Biology}, year={2012}, volume={15}, pages={376-383} }
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… CONTINUE READING
Figures, Tables, and Topics from this paper
34 Citations
Characterization of [11C]Cimbi-36 as an agonist PET radioligand for the 5-HT2A and 5-HT2C receptors in the nonhuman primate brain
- Chemistry, Medicine
- NeuroImage
- 2014
- 44
Serotonin 2A Receptor Agonist Binding in the Human Brain with [11C]Cimbi-36
- Chemistry, Medicine
- Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
- 2014
- 62
Human biodistribution and radiation dosimetry of the 5-HT2A receptor agonist Cimbi-36 labeled with carbon-11 in two positions
- Medicine
- EJNMMI Research
- 2019
- 1
In vivo evaluation of [18F]FECIMBI-36, an agonist 5-HT2A/2C receptor PET radioligand in nonhuman primate.
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 2017
- 5
Serotonin 2A receptor agonist binding in the human brain with [11C]Cimbi-36: Test–retest reproducibility and head-to-head comparison with the antagonist [18F]altanserin
- Medicine, Computer Science
- NeuroImage
- 2016
- 38
Synthesis and in vitro evaluation of [18F]FECIMBI-36: A potential agonist PET ligand for 5-HT2A/2C receptors.
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 2015
- 8
Current radiosynthesis strategies for 5-HT2A receptor PET tracers.
- Chemistry, Medicine
- Journal of labelled compounds & radiopharmaceuticals
- 2015
- 9
Hunting for the high‐affinity state of G‐protein‐coupled receptors with agonist tracers: Theoretical and practical considerations for positron emission tomography imaging
- Chemistry, Medicine
- Medicinal research reviews
- 2019
- 11
- PDF
Correlating the Metabolic Stability of Psychedelic 5-HT2A Agonists with Anecdotal Reports of Human Oral Bioavailability
- Chemistry, Medicine
- Neurochemical Research
- 2014
- 11
Synthesis and structure-activity relationships of N-benzyl phenethylamines as 5-HT2A/2C agonists.
- Chemistry, Medicine
- ACS chemical neuroscience
- 2014
- 62
References
SHOWING 1-10 OF 20 REFERENCES
Radiosynthesis and Evaluation of 11C-CIMBI-5 as a 5-HT2A Receptor Agonist Radioligand for PET
- Chemistry, Medicine
- The Journal of Nuclear Medicine
- 2010
- 38
- PDF
Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers
- Chemistry, Medicine
- European Journal of Nuclear Medicine and Molecular Imaging
- 2010
- 87
- PDF
Characterization of in vivo pharmacological properties and sensitivity to endogenous serotonin of [11C] P943: A positron emission tomography study in Papio anubis
- Chemistry, Medicine
- Synapse
- 2011
- 24
In vitro and in vivo characterisation of [11C]-DASB: a probe for in vivo measurements of the serotonin transporter by positron emission tomography.
- Chemistry, Medicine
- Nuclear medicine and biology
- 2002
- 138
Confirmation of Fenfluramine Effect on 5-HT1B Receptor Binding of [11C]AZ10419369 using an Equilibrium Approach
- Chemistry, Medicine
- Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
- 2012
- 35
- PDF
A Comparative Evaluation of the Dopamine D2/3 Agonist Radiotracer [11C](−)-N-Propyl-norapomorphine and Antagonist [11C]Raclopride to Measure Amphetamine-Induced Dopamine Release in the Human Striatum
- Chemistry, Medicine
- Journal of Pharmacology and Experimental Therapeutics
- 2010
- 73
- PDF
No change in [11C]CUMI‐101 binding to 5‐HT1A receptors after intravenous citalopram in human
- Chemistry, Medicine
- Synapse
- 2012
- 29
Measurement of the Proportion of D2 Receptors Configured in State of High Affinity for Agonists in Vivo: A Positron Emission Tomography Study Using [11C]N-Propyl-norapomorphine and [11C]Raclopride in Baboons
- Chemistry, Medicine
- Journal of Pharmacology and Experimental Therapeutics
- 2005
- 54
- PDF
Measuring Endogenous 5-HT Release by Emission Tomography: Promises and Pitfalls
- Psychology, Medicine
- Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
- 2010
- 121
- PDF
Multiple conformations of native and recombinant human 5-hydroxytryptamine(2a) receptors are labeled by agonists and discriminated by antagonists.
- Chemistry, Medicine
- Molecular pharmacology
- 2001
- 43