automated-radiochemical-synthesis-18f3f4ap-novel-pet-tracer-for

Automated Radiochemical Synthesis of [<sup>18</sup>F]3F4AP: A Novel PET Tracer for Imaging Demyelinating Diseases

3-[18F]fluoro-4-aminopyridine, [18F]3F4AP, is a radiofluorinated analog of the FDA-approved drug for multiple sclerosis 4-aminopyridine (4AP). This ...

The University of Chicago

A high-sensitivity, high-resolution brain PET scanner ("G-PET") has been developed. This scanner is similar in geometry to a previous brain scanner developed at the University of Pennsylvania, the HEAD Penn-PET, but the detector technology and electronics have been improved to achieve enhanced performance.

Performance of a brain PET camera based on anger-logic gadolinium oxyorthosilicate detectors.

To assess the accuracy of 18F-fluoro-L-dihydroxyphenylalanine ([18F]-DOPA) PET scans to diagnose focal versus diffuse disease and to localize focal lesions in infants with congenital hyperinsulinism.

Diagnosis and localization of focal congenital hyperinsulinism by 18F-fluorodopa PET scan.

Focal lesions in infants with congenital hyperinsulinism (HI) represent areas of adenomatosis that express a paternally derived ATP-sensitive potassium channel mutation due to embryonic loss of heterozygosity for the maternal 11p region. This study evaluated the accuracy of 18F-fluoro-l-dihydroxyphenylalanine ([18F]DOPA) positron emission tomography (PET) scans in diagnosing focal vs. diffuse disease and identifying the location of focal lesions.

Accuracy of [18F]fluorodopa positron emission tomography for diagnosing and localizing focal congenital hyperinsulinism.

We acquire and compare three-dimensional tomographic breast images of three females with suspicious masses using diffuse optical tomography (DOT) and positron emission tomography (PET). Co-registration of DOT and PET images was facilitated by a mutual information maximization algorithm. We also compared DOT and whole-body PET images of 14 patients with breast abnormalities. Positive correlations were found between total hemoglobin concentration and tissue scattering measured by DOT, and fluorodeoxyglucose (18F-FDG) uptake. In light of these observations, we suggest potential benefits of combining both PET and DOT for characterization of breast lesions.

Comparison of diffuse optical tomography of human breast with whole-body and breast-only positron emission tomography.

11C-carfentanil is a radiopharmaceutical that selectively binds the mu-opiate receptor of the central nervous system. However, its dosimetry throughout the body and other organs has never been reported in the literature. The purpose of this study was to measure the radiation dosimetry of 11C-carfentanil in healthy human volunteers. The study was conducted within a regulatory framework that required its pharmacological safety to be assessed simultaneously.

Dosimetry of 11C-carfentanil, a micro-opioid receptor imaging agent.

Tumour hypoxia affects cancer biology and therapy-resistance in both animals and humans. The purpose of this study was to determine whether EF5 ([2-(2-nitro-1-H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl)-acetamide]) binding and/or radioactive drug uptake correlated with single-dose radiation response in 9L gliosarcoma tumours.

The radiation response of cells from 9L gliosarcoma tumours is correlated with [F18]-EF5 uptake.

The primary purpose of this study was to assess the biodistribution and radiation dose resulting from administration of (18)F-EF5, a lipophilic 2-nitroimidazole hypoxia marker in ten cancer patients. For three of these patients (with glioblastoma) unlabeled EF5 was additionally administered to allow the comparative assessment of (18)F-EF5 tumor uptake with EF5 binding, the latter measured in tumor biopsies by fluorescent anti-EF5 monoclonal antibodies.

Biodistribution and dosimetry of (18)F-EF5 in cancer patients with preliminary comparison of (18)F-EF5 uptake versus EF5 binding in human glioblastoma.

Reverse cholesterol transport (RCT) is thought to be an atheroprotective function of HDL, and macrophage-specific RCT in mice is inversely associated with atherosclerosis. We developed a novel method using (3)H-cholesterol nanoparticles to selectively trace macrophage-specific RCT in vivo in humans. Use of (3)H-cholesterol nanoparticles was initially tested in mice to assess the distribution of tracer and response to interventions known to increase RCT. Thirty healthy subjects received (3)H-cholesterol nanoparticles intravenously, followed by blood and stool sample collection. Tracer counts were assessed in plasma, nonHDL, HDL, and fecal fractions. Data were analyzed by using multicompartmental modeling. Administration of (3)H-cholesterol nanoparticles preferentially labeled macrophages of the reticuloendothelial system in mice, and counts were increased in mice treated with a liver X receptor agonist or reconstituted HDL, as compared with controls. In humans, tracer disappeared from plasma rapidly after injection of nanoparticles, followed by reappearance in HDL and nonHDL fractions. Counts present as free cholesterol increased rapidly and linearly in the first 240 min after nadir; counts in cholesteryl ester increased steadily over time. Estimates of fractional transfer rates of key RCT steps were obtained. These results support the use of (3)H-cholesterol nanoparticles as a feasible approach for the measurement of macrophage RCT in vivo in humans.

Article	Year
Performance of a brain PET camera based on anger-logic gadolinium oxyorthosilicate detectors. Journal of nuclear medicine : official publication, Society of Nuclear Medicine\| PubMed ID: 12902426	2003
Diagnosis and localization of focal congenital hyperinsulinism by 18F-fluorodopa PET scan. The Journal of pediatrics\| PubMed ID: 17236890	2007
Accuracy of [18F]fluorodopa positron emission tomography for diagnosing and localizing focal congenital hyperinsulinism. The Journal of clinical endocrinology and metabolism\| PubMed ID: 17895314	2007
Comparison of diffuse optical tomography of human breast with whole-body and breast-only positron emission tomography. Medical physics\| PubMed ID: 18383664	2008
Dosimetry of 11C-carfentanil, a micro-opioid receptor imaging agent. Nuclear medicine communications\| PubMed ID: 19242386	2009
The radiation response of cells from 9L gliosarcoma tumours is correlated with [F18]-EF5 uptake. International journal of radiation biology\| PubMed ID: 19995239	2009
Biodistribution and dosimetry of (18)F-EF5 in cancer patients with preliminary comparison of (18)F-EF5 uptake versus EF5 binding in human glioblastoma. European journal of nuclear medicine and molecular imaging\| PubMed ID: 20585774	2010
A novel approach to measuring macrophage-specific reverse cholesterol transport in vivo in humans. Journal of lipid research\| PubMed ID: 28167703	2017

Richard Freifelder

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