We investigated the age-related changes of the binding of [11C]CFT to striatal dopamine transporters (DATs) in vivo in Fischer 344 rats by positron emission tomography (PET). The tissue dissection method represented an age-related decrease in the uptake ratio of the striatum to the cerebellum and in the specific binding-to-nonspecific binding ratio of [11C]CFT. PET demonstrated an age-dependent...

The aim of this study was to investigate the efficacy of 11C-choline PET/CT imaging for lung cancer and the correlation between choline uptake of lung cancer tissue and the expression of choline kinase (ChoK), phosphorylcholine-cytidyl transferase and Ki-67 index. Between March 2008 and June 2010, 53 patients diagnosed or suspected of having lung ...

BACKGROUND Serotonin 5-HT4 receptor (5-HT4-R) agonists are potential therapeutic agents for enterokinetic and cognitive disorders and are marketed for treatment of constipation. The aim of this study was to develop an agonist positron emission tomography (PET) ligand in order to label the active G-protein coupled 5-HT4-R in peripheral and central tissues. For this purpose prucalopride, a high-a...

Inflammatory/immunological process and glial contribution are suggested in the pathophysiology of schizophrenia. We investigated peripheral benzodiazepine receptors in brains of patients with chronic schizophrenia, which were reported to be located on mitochondria of glial cells, using [11C]DAA1106 with positron emission tomography. Fourteen patients and 14 age- and sex-matched normal controls ...

Hyperthermia-induced metabolic changes in tumor tissue have been monitored by PET. Uptake of L-[1-11C]tyrosine in rhabdomyosarcoma tissue of Wag/Rij rats was dose-dependently reduced after local hyperthermia treatment at 42, 45, or 47 degrees C. Tumor blood flow, as measured by PET with 13NH3, appeared to be unchanged. The L-[1-11C]tyrosine uptake data were compared to uptake data of L-[1-14C]t...

NPS 1506 [3-fluoro-gamma-(3-fluorophenyl)-N-methylbenzenepropamine] is representative of a non-psychotomimetic class of N-methyl-D-aspartate (NMDA) receptor antagonists. [11C]NPS 1506 was prepared at high radiochemical purity (>98%) with a specific activity of around 50 GBq/micromol at the end of synthesis by methylation of the desmethyl precursor with [11C]methyl iodide in the presence of NaH....

The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci/µmol, n=5). Evaluation of [11C]PBD150 by small animal PET imaging (mouse and rat) determined it does not permeate the blood brain barrier, ...

Tumor cells can be selectively killed by application of s-ligands; high concentrations (20–100 mM) are often required, however, because either diffusion barriers must be passed to reach intracellular sites or the entire s-receptor population should be occupied to induce cell death. We measured receptor occupancies associated with the cytotoxic effect and dose-dependent changes of cellular metab...

The aim of this study was to compare 11C-choline PET/CT and bone scintigraphy (BS) for detection of bone metastases in patients with prostate cancer. Twenty-one patients with histologically proven prostate cancer underwent 11C-choline PET/CT and BS before (n = 4) or after (n = 17) treatment. Patient-, region-, and lesion-based diagnostic performances of bone metastasis of both 11C-choline PET/C...

Brain -opioid receptors (ORs) may be involved in several pathologic conditions, such as addiction, psychosis, and seizures. ( )-4-Methoxycarbonyl-2-[(1-pyrrolidinylmethyl]-1-[(3,4dichlorophenyl)acetyl]-piperidine (GR89696) is a potent and selective -OR agonist. The ( )-isomer, GR103545, is the active enantiomer of GR89696. The aim of this study was to characterize the potential of 11C-GR103545 ...