Fully Automated Methods for [F]FDG and [F]-NaF Productions Using Explora FDG4: Validation and Reliability of Multi-subsequent Preparations for Clinical Applications.

Background: The worldwide usage of [F]-sodium fluoride in clinical applications has increased the interest in the facility of its production. The development of a new automated method for multi-preparations of [F]-NaF and [F]FDG on an Explora FDG4 module is described. Explora FDG4 is one of the most widely used synthesizers for FDG production in daily routine use and is specifically designed to run up to four different productions with a single module.

Fluorine walk: The impact of fluorine in quinolone amides on their activity against African sleeping sickness.

Human African Trypanosomiasis, also known as African sleeping sickness, is caused by the parasitic protozoa of the genus Trypanosoma. If there is no pharmacological intervention, the parasites can cross the blood-brain barrier (BBB), inevitably leading to death of the patients. Previous investigation identified the quinolone amide GHQ168 as a promising lead compound having a nanomolar activity against T.

Initial Clinical Investigation of [18F]Tetrafluoroborate PET/CT in Comparison to [124I]Iodine PET/CT for Imaging Thyroid Cancer.

Aim: Recently, [F]tetrafluoroborate ([F]TFB) has been introduced as a versatile PET probe for imaging the human sodium/iodide symporter activity. This pilot study aimed to compare [F]TFB-PET/CT with [I]NaI-PET/CT imaging in thyroid cancer patients.

Methods: Nine patients with newly diagnosed differentiated thyroid cancer underwent both [F]TFB- and [I]NaI-PET/CT after total thyroidectomy.

Validation of a [AlF]PSMA-11 preparation for clinical applications.

Unlabelled: Imaging prostate-specific membrane antigen (PSMA) using positron emission tomography (PET) has been presented so far as the most sensitive and specific with regard to prostate cancer detection, in particular in high-risk prostate cancer patients. Currently, it mainly features Gallium-68 (Ga) labeled PSMA ligands, notably [Ga]Glu-urea-Lys(Ahx)-HBED-CC ([Ga]-PSMA-11) and [Ga]DOTAGA-FFK (Sub-KuE termed ([Ga]PSMA-I&T). However, Ga has several shortcomings as radionuclide including a short half-life and non-ideal energies.

Cholinergic activity and levodopa-induced dyskinesia: a multitracer molecular imaging study.

Objective: To investigate the association between levodopa-induced dyskinesias and striatal cholinergic activity in patients with Parkinson's disease.

Methods: This study included 13 Parkinson's disease patients with peak-of-dose levodopa-induced dyskinesias, 12 nondyskinetic patients, and 12 healthy controls. Participants underwent 5-[I]iodo-3-[2(S)-2-azetidinylmethoxy]pyridine single-photon emission computed tomography, a marker of nicotinic acetylcholine receptors, [I]N--fluoropropyl-2-carbomethoxy-3-(4-iodophenyl)nortropane single-photon emission computed tomography, to measure dopamine reuptake transporter density and 2-[F]fluoro-2-deoxyglucose positron emission tomography to assess regional cerebral metabolic activity.

A Novel Way To Radiolabel Human Butyrylcholinesterase for Positron Emission Tomography through Irreversible Transfer of the Radiolabeled Moiety.

The enzyme butyrylcholinesterase (BChE) is known to be involved in the detoxification of xenobiotics in blood plasma and is associated with the progress of neurodegenerative disorders, diabetes type 2, obesity, and diseases of the cardiovascular system. In the present study, we developed carbamate-based inhibitors serving as positron emission tomography (PET) radiotracers with (18) F and (11) C as radioisotopes to visualize BChE distribution. These inhibitors are radiolabeled at the carbamate site and transfer this moiety onto BChE, which thus results in covalent and permanent radiolabeling of the enzyme.

Combined [(18)F]DPA-714 micro-positron emission tomography and autoradiography imaging of microglia activation after closed head injury in mice.

Background: Traumatic brain injury (TBI) is a major cause of death and disability. Neuroinflammation contributes to acute damage after TBI and modulates long-term evolution of degenerative and regenerative responses to injury. The aim of the present study was to evaluate the relationship of microglia activation to trauma severity, brain energy metabolism, and cellular reactions to injury in a mouse closed head injury model using combined in vivo PET imaging, ex vivo autoradiography, and immunohistochemistry.

Improved synthesis of [¹⁸F]FS-PTAD as a new tyrosine-specific prosthetic group for radiofluorination of biomolecules.

A novel prosthetic group, 4-(p-([(18)F]fluorosulfonyl)phenyl)-1,2,4-triazoline-3,5-dione ([(18)F]FS-PTAD) for site-specific radiofluorination of tyrosine residue in small molecules is described. Coupling of [(18)F]FS-PTAD with L-tyrosine, N-acetyl-L-tyrosine methyl amide and phenol as model compounds were achieved in buffered aqueous solution at room temperature, resulting in the corresponding fluorinated tyrosine and phenol derivatives. The total synthesis time including radiosynthesis, HPLC purification and formulation was less than 60 min (n=15) with ≥98% radio chemical purity.

Synthesis and biological activity of some 3-(4-(substituted)-piperazin-1-yl)cinnolines.

A new series of 6-substituted-4-methyl-3-(4-arylpiperazin-1-yl)cinnolines 8-10 were synthesized as potential antifungal agents via intramolecular cyclization of the respective 1-(2-arylhydrazono)-1-(4-arylpiperazin-1-yl)propan-2-ones 5-7, mediated by polyphosphoric acid (PPA). The amidrazones themselves were synthesized via direct interaction of the appropriate hydrazonoyl chlorides 4a-d with the corresponding N-substituted piperazine in the presence of triethylamine. The structures of the new prepared compounds were confirmed by elemental analyses, (1)H-NMR, (13)C-NMR, and ESI-HRMS spectral data.

Auger electron emitter against multiple myeloma--targeted endo-radio-therapy with 125I-labeled thymidine analogue 5-iodo-4'-thio-2'-deoxyuridine.

Introduction: Multiple myeloma (MM) is a plasma cell malignancy characterized by accumulation of malignant, terminally differentiated B cells in the bone marrow. Despite advances in therapy, MM remains an incurable disease. Novel therapeutic approaches are, therefore, urgently needed.

New molecular markers for prostate tumor imaging: a study on 2-methylene substituted fatty acids as new AMACR inhibitors.

The development of prostate carcinoma is associated with alterations in fatty acid metabolism. α-Methylacyl-CoA racemase (AMACR) is a peroxisomal and mitochondrial enzyme that catalyses interconversion between the (S)/(R)-isomers of a range of α-methylacyl-CoA thioesters. AMACR is involved in the β-oxidation of the dietary branched-chain fatty acids and bile acid intermediates.