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Cannabinoid receptor type 2 (CB2) as one of the candidate genes in human carotid plaque imaging: Evaluation of the novel radiotracer [11C]RS-016 targeting CB2 in atherosclerosis.
Preclinical imaging of the co-stimulatory molecules CD80 and CD86 with indium-111-labeled belatacept in atherosclerosis
- Romana Meletta, Adrienne Müller Herde, P. Dennler, E. Fischer, R. Schibli, S. Krämer
- Biology, MedicineEJNMMI Research
- 4 January 2016
DOTA-belatacept accumulates in CD80/CD86-positive tissues in vivo and in vitro rendering it a research tool for the assessment of inflammatory activity in atherosclerosis and possibly other diseases.
Evaluation of the Radiolabeled Boronic Acid-Based FAP Inhibitor MIP-1232 for Atherosclerotic Plaque Imaging
Target expression analyses revealed a moderately higher protein level in atherosclerotic plaques than normal arteries correlating with plaque vulnerability, and binding of the tracer to endarterectomized tissue was similar in plaques and normal arteries, hampering its use for atherosclerosis imaging.
Quantitative positron emission tomography of mGluR5 in rat brain with [18F]PSS232 at minimal invasiveness and reduced model complexity
This work aimed at minimizing invasiveness of IF recording in rat and employing this protocol for mGluR5 quantitative PET with [18F]PSS232, an F‐18‐labeled analog of the mGLUR5‐targeting [11C]ABP688, and defining models of low complexity for quantitativePET with [ 18F] PSS232.
Chronic Nicotine Exposure Alters Metabotropic Glutamate Receptor 5: Longitudinal PET Study and Behavioural Assessment in Rats
It is demonstrated that chronic nicotine administration alters behaviour and mGluR5 availability and Chronic nicotine administration leads to decreased [18F]PSS232 binding which normalizes after prolonged nicotine withdrawal.
Synthesis and Pharmacological Evaluation of [11C]Granisetron and [18F]Fluoropalonosetron as PET Probes for 5-HT3 Receptor Imaging.
PET experiments suggested that [18F]15 and [11C]2 are of limited utility for the PET imaging of brain 5-HT3 receptors in vivo, while in vitro autoradiography with both compounds revealed a heterogeneous and displaceable binding in cortical and hippocampal regions that are known to express 5- HT3 receptors at significant levels.
Discovery of a high affinity and selective pyridine analog as a potential positron emission tomography imaging agent for cannabinoid type 2 receptor.
2,5,6-substituted pyridines as a novel class of potential CB2 PET ligands investigated for their potency and binding properties toward human and rodent CB1 and CB2 and 16 is a promising radiotracer for imaging CB2 in rodents.
Synthesis and Biological Evaluation of Thiophene-Based Cannabinoid Receptor Type 2 Radiotracers for PET Imaging
- A. Haider, Adrienne Müller Herde, Simon Mensah Ametamey
- Biology, ChemistryFront. Neurosci.
- 27 July 2016
The obtained results revealed unspecific binding in spleen tissue that was not blocked by an excess of CB2-specific ligand GW402833, and a suitable positron emission tomography tracer to visualize the CB2 receptor in patients suffering from neurodegenerative diseases is developed.
Novel chemoselective (18)F-radiolabeling of thiol-containing biomolecules under mild aqueous conditions.
We report a novel prosthetic group based on a heterocyclic methylsulfone derivative for the rapid, stable, and chemoselective (18)F-labeling of thiol-containing (bio)molecules under mild aqueous…
Discovery of a fluorinated 4‐oxo‐quinoline derivative as a potential positron emission tomography radiotracer for imaging cannabinoid receptor type 2
Three novel fluorinated analogs of RS‐126 demonstrated high specificity toward CB2 receptor in vitro and in vivo and is a promising radioligand for imagingCB2 receptor expression.