Expanding PET-applications in life sciences with positron-emitters beyond fluorine-18.

Positron-emission-tomography (PET) has become an indispensable diagnostic tool in modern nuclear medicine. Its outstanding molecular imaging features allow repetitive studies on one individual and with high sensitivity, though no interference. Rather few positron-emitters with near favourable physical properties, i.

Current trends in the use of O-(2-[F]fluoroethyl)-L-tyrosine ([F]FET) in neurooncology.

The diagnostic potential of PET using the amino acid analogue O-(2-[F]fluoroethyl)-L-tyrosine ([F]FET) in brain tumor diagnostics has been proven in many studies during the last two decades and is still the subject of multiple studies every year. In addition to standard magnetic resonance imaging (MRI), positron emission tomography (PET) using [F]FET provides important diagnostic data concerning brain tumor delineation, therapy planning, treatment monitoring, and improved differentiation between treatment-related changes and tumor recurrence. The pharmacokinetics, uptake mechanisms and metabolism have been well described in various preclinical studies.

Baeyer-Villiger oxidation tuned to chemoselective conversion of non-activated [ F]fluorobenzaldehydes to [ F]fluorophenols.

A reaction pathway via oxidation of [ F]fluorobenzaldehydes offers a very useful tool for the no-carrier-added radiosynthesis of [ F]fluorophenols, a structural motive of several potential radiopharmaceuticals. A considerably improved chemoselectivity of the Baeyer-Villiger oxidation (BVO) towards phenols was achieved, employing 2,2,2-trifluoroethanol as reaction solvent in combination with Oxone or m-CPBA as oxidation agent. The studies showed the necessity of H SO addition, which appears to have a dual effect, acting as catalyst and desiccant.

Cis-4-[18F]fluoro-D-proline detects neurodegeneration in patients with akinetic-rigid parkinsonism.

Objectives: This study aimed to investigate whether the amino acid PET tracer cis-4-[F]fluoro-D-proline [D-cis-[F]FPro] shows increased uptake in the basal ganglia of patients with neurodegenerative akinetic-rigid parkinsonism. D-Cis-[F]FPro is a sensitive PET tracer for inflammation-associated neurodegeneration in animal models. We hypothesized that D-cis-[F]FPro might also be a sensitive marker of alterations of the basal ganglia in parkinsonian syndromes.

Treatment-Related Uptake of -(2-F-Fluoroethyl)-l-Tyrosine and l-[Methyl-H]-Methionine After Tumor Resection in Rat Glioma Models.

Assessment of residual tumor after resection of cerebral gliomas can be difficult with MRI and may be improved by amino acid PET. The aim of this experimental study was to investigate uptake of 2-F-fluoroethyl-l-tyrosine (F-FET) and l-[methyl-H]-methionine (H-MET) in residual tumor after surgery and possible false-positive uptake in treatment-related changes. F98 or GS-9L rat gliomas were implanted into the brain of 64 rats.

Mn-Labelled CDTA-based trimeric complexes as novel bimodal PET/MR probes with high relaxivity.

trans-1,2-Diaminocyclohexane-N,N,N',N'-tetraacetic acid (CDTA) labelled with a mixture of paramagnetic 55Mn(ii) and β+-emitting 52gMn(ii) offers access to bimodal Positron Emission Tomography/Magnetic Resonance (PET/MR) tracers. To enhance the number of NMR-active nuclei and simultaneously improve the longitudinal relaxivity r1, a complex composed of three CDTA units was designed. Accordingly, a functionalised tris-CDTA-1,3,5-tris-triazolobenzene was prepared and labelled with c.

Consensus nomenclature rules for radiopharmaceutical chemistry - Setting the record straight.

Over recent years, within the community of radiopharmaceutical sciences, there has been an increased incidence of incorrect usage of established scientific terms and conventions, and even the emergence of 'self-invented' terms. In order to address these concerns, an international Working Group on 'Nomenclature in Radiopharmaceutical Chemistry and related areas' was established in 2015 to achieve clarification of terms and to generate consensus on the utilisation of a standardised nomenclature pertinent to the field. Upon open consultation, the following consensus guidelines were agreed, which aim to.

Novel CDTA-based, Bifunctional Chelators for Stable and Inert Mn Complexation: Synthesis and Physicochemical Characterization.

In the search for Mn MR and PET/MR imaging agents with optimal balance between thermodynamic stability, kinetic inertness, and relaxivity, two novel bifunctional Mn chelators (BFMnCs) based on CDTA (trans-1,2-diaminocyclohexane-N,N,N',N'-tetraacetic acid) were synthesized. A six-step synthesis, involving the buildup of a functionalized trans-1,2-diaminocyclohexane core, provided CuAAC-reactive 6a and 6b bearing an alkyne or azide substituent on the cyclohexane ring, respectively (CuAAC = Cu-catalyzed azide-alkyne 1,3-dipolar cycloaddition). Thermodynamic, kinetic, and relaxometric studies were performed with 4-HET-CDTA (8a) as a "model chelator," synthesized in two steps from 6a.

Efficient synthesis of [ F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols.

An improved high yielding radiosynthesis of the known thiol-reactive maleimide-containing prosthetic group1-[3-(2-[ F]fluoropyridine-3-yloxy)propyl]pyrrole-2,5-dione ([ F]FPyME) is described. The target compound was obtained by a two-step one-pot procedure starting from a maleimide-containing nitro-precursor that was protected as a Diels-Alder adduct with 2,5-dimethylfurane. Nucleophilic radiofluorination followed by heat induced deprotection through a Retro Diels Alder reaction yielded, after chromatographic isolation, [ F]FPyME with a radiochemical yield of 20% in about 60 min overall synthesis time.

New potent A adenosine receptor radioligands for positron emission tomography.

8-Cyclopentyl-3-(3-[F]fluoropropyl)-1-propylxanthine ([F]CPFPX) is meanwhile an accepted receptor ligand to examine the A adenosine receptor (AAR) in humans by positron emission tomography (PET). A major drawback of this compound is its rather fast metabolic degradation in vivo. Therefore two new xanthine derivatives, namely 8-cyclobutyl-1-cyclopropymethyl-3-(3-fluoropropyl)xanthine (CBCPM; 5) and 1-cyclopropylmethyl-3-(3-fluoropropyl)-8-(1-methylcyclobutyl)xanthine (CPMMCB; 6) were designed and synthesized as potential alternatives to CPFPX.

Synthesis of a Potent Aminopyridine-Based nNOS-Inhibitor by Two Recent No-Carrier-Added (18)F-Labelling Methods.

Nitric oxide (NO), an important multifunctional signaling molecule, is produced by three isoforms of NO-synthase (NOS) and has been associated with neurodegenerative disorders. Selective inhibitors of the subtypes iNOS (inducible) or nNOS (neuronal) are of great interest for decoding neurodestructive key factors, and (18)F-labelled analogues would allow investigating the NOS-function by molecular imaging with positron emission tomography. Especially, the highly selective nNOS inhibitor 6-((3-((3-fluorophenethylamino)methyl)phenoxy)methyl)-4-methylpyridin-2-amine (10) lends itself as suitable compound to be (18)F-labelled in no-carrier-added (n.

Circadian variation of metabotropic glutamate receptor 5 availability in the rat brain.

The metabotrophic subtype 5 glutamate receptor (mGluR5) plays a critical role in synaptic plasticity besides its involvement in numerous neurological disorders, such as depression. As mGluR5 availability in humans is altered in sleep deprivation, we hypothesized that mGluR5 availability underlies a circadian variation. To investigate whether mGluR5 underlies potential circadian changes we measured its density in a randomized fashion at six different daytimes in 11 adult Sprague-Dawley rats.

[German Society of Nuclear Medicine procedure guideline on beta-amyloid brain PET imaging].

Recently, a number of positron emission tomography (PET) radiotracers have been approved for clinical use. These tracers target cerebral beta-amyloid (Aβ) plaques, a hallmark of Alzheimer's disease. Increasing use of this method implies the need for respective standards.