Franz Oberdorfer

• Doctor of Philosophy
• Managing Director at Zyklotron AG

Introduction: Good manufacturing practice (GMP)-compliant production of radiopharmaceuticals for parenteral application requires great efforts in maintenance of clean room infrastructure and equipment in order to reliably guarantee the constant hygienic quality of the product (sterility). Terminal sterilization of the product is not always possibl...

Positron emission tomography (PET) is a noninvasive functional method for the study of solid tumor perfusion, metabolism and interaction with different therapeutic agents. The aim of the study was the investigation of the metabolism of hepatocellular carcinomas (HCC) and the kinetics during a treatment with intratumoral ethanol by PET. The ongoing...

[11C]Lithium trimethylsilyl ynolate was characterized to be a new precursor in carbon-11 chemistry. It was obtained from [11C]carbon monoxide and lithiated silyldiazomethane. The new precursor might be of high potential for the incorporation of carbon 11 into heterocyclic ring systems for which labeling methods are not well developed. More examples...

[11C]Lithium trimethylsilyl ynolate was characterized to be a new precursor in carbon-11 chemistry. It was obtained from [11C]carbon monoxide and lithiated silyldiazomethane. The new precursor might be of high potential for the incorporation of carbon 11 into heterocyclic ring systems for which labeling methods are not well developed. More examples...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

The reaction of pyridine with ditechnetium decacarbonyl [Tc2(CO)10] (1) leads to a novel ortho-pyridyl-ditechnetium hydrido complex, [Tc2(mu-H)(mu-NC5H4)(NC5H5)2(CO)6] (2) and its precursor [Tc2(mu-CO)2(NC5H5)2(CO)6] (3). At ambient temperature 1 was found to react slowly with pyridine to afford the substitution product 3 after 120 h. However, heat...

2-Deoxy-2-[18 F] fluoro-D-galactose was prepared using gaseous [18F]acetyl hypofluorite or [18F]F2 and tri-O-acetyl-D-galactal as substrate. The product was obtained in a surprisingly high epimeric purity (>90%), even with [18F]F2 as fluorinating reagent, as demonstrated by HPLC and high-resolution 1H- and 19F-NMR spectroscopy. This is the first re...

5(S)-Hydroxy-6(R)-(N-[1-11C]acetyl)cysteinyl-7,9-trans-11,14-cis-eicosatetraenoic acid (N-[1-11C]acetyl leukotriene E4) was prepared by the reaction of leukotriene E4 and [1-11C]acetyl chloride. The product was obtained with 1.3% yield, based on [1-11C]acetyl chloride. The preparation required 50 min from the end of radioisotope production. The che...

A virtually planar water tetramer in which the water molecules are virtually tetrahedrally coordinated could be realized in the solid in a three-dimensional network of [Tc4(CO)12-(mu3-OH)4.4H2O]. The network could be produced by cocrystallization of the new cubane-like cluster [Tc(CO)3-(mu3-OH)]4 and water as a complementary component. The amphiphi...

For Abstract see ChemInform Abstract in Full Text.

Syntheses of 5-(2-[18F]fluoroethyl)- (1), 5-(2-[80Br]bromoethyl)- (2), un-deprotected (E)-5-(2-[18F]fluorovinyl)- (3) and (E)-5-(2-[80Br]bromovinyl)-2′-deoxyuridines (4) as the tracers for monitoring cancer gene therapy with positron emission tomography were described. Decay corrected radiochemical yield and synthesis time including labeling and HP...

For Abstract see ChemInform Abstract in Full Text.

The synthesis of the blocked nucleoside 3',5'-di-O-p-toluoyl-4-O-methyl-5-formylmethyl-2'-deoxyuridine was accomplishied in eleven steps from gamma-butyrolactone. This aldehyde, which should facilitate the synthesis of nucleosides containing 18F. was converted to the corresponding blocked dithianyl nucleoside, and also to 5-(2,2-difluoroethyl)-subs...

A solid phase technique for the preparation of antisense oligodeoxynucleotides (ODNs) is described featuring 5'-end conjugated 4-[(1,4,8,11-tetraazacyclotetradec-1-yl)-methyl]benzoic acid (CPTA). Using Fmoc-protected CPTA-C6 amidite, CPTA was conjugated to ODNs at the end of an automated DNA synthesis. To illustrate successful conjugations, the CPT...

Syntheses of [carbonyl-11C]2-(2-benzoylphenoxy)-N-phenylacetamide, a radiolabeled inhibitor of human immunodeficiency virus type 1 (HIV 1) reverse transcriptase, were achieved by applying palladium-mediated cross-coupling reactions with insertion of [11C]carbon monoxide. Our interest was focused for the present on a comparison of the Stille and Suz...

eight tumors. CONCLUSION: Inhomogeneous drug distribution and drug dilution in the target area are likely to be the major limiting parameters for therapy response. Percutaneous ethanol injection is used for curative or palliative treatment of hepatocellular carcinomas. Percutaneous ethanol injection is considered a reliable alternative to surgical...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

The usefulness of 18F-labelled carbohydrates, especially 2-deoxy-2-[18F]fluoro-D-glucose, to study pathophysiological processes in man non-invasively using positron-emission-tomography (PET) led to a widespread investigation of different 18F-labelled sugars and sugar derivatives. In consideration of the short half-life of fluorine-18 (T(1/2) = 110...

The dramatic expansion of clinical gene therapy trials requires the development of noninvasive clinical monitoring procedures, which provide information about expression levels, expression kinetics, and spatial distribution of transduced therapeutic genes. With the development of such procedures, invasive sampling of tissue probes from patients pot...

The aim of the study was the evaluation of the detectability of treated liver metastases using one FDG-PET measurement. The study includes 42 patients (80 lesions) from different primary tumours. Standardized Uptake Values (SUV) as well as the tumour to liver Ratio (T/L) were used for evaluation. A T/L > 1.0 was considered to be pathological. Clini...

To evaluate the carbon 11 ethanol kinetics with positron emission tomography after intratumoral injection of the tracer and assess its redistribution and dilution in patients who have hepatocellular carcinomas and who were scheduled for treatment with percutaneous ethanol injection. The study included eight patients with hepatocellular carcinomas....

Recently, MR-imaging techniques have been developed to quantify radiation doses with use of Fricke-gels. Fricke-gel-dosimetry requires a precise measurement of longitudinal relaxation rates R1. In this study two MR-methods for R1-determination of irradiated Fricke-gels were compared using a spinecho- and a TurboFLASH-technique. R1 measurements were...

A comparative study has been performed on the selective reduction of cyclotron-produced [11C]carbon dioxide to [11C]formaldehyde with solutions of various complex metal hydrides at temperatures between −52 and +25°C. Under optimal reaction conditions, lithium tetrahydridoaluminate gave the highest yield of [11C]formaldehyde (58%, decay-corrected),...

Prediction of chemotherapy response is still a problem in oncological patients. Studies with PET and 18F-fluorouracil (FU) were used for measurements of drug concentrations in patients with liver metastases from colorectal carcinoma. The PET data obtained before onset of FU chemotherapy were correlated to the growth rate of the metastases after the...

Intra-arterial chemotherapy can potentially increase drug delivery at the tumor sites and has therefore been used for the therapy of metastatic colorectal cancer. Dynamic PET and [18F]fluorouracil (18F-FU) were used in patients with liver metastases from colorectal cancer to examine the pharmacokinetics of the drug up to 120 min after intravenous a...

D-Galactal 1 reacts in THF in the presence of catalytic amounts of concentrated sulfuric acid to give (2R)-2-hydroxy-6,8-dioxabicyclo[3.2.1]oct- 3-ene (4) in a Ferrier-type rearrangement in 40% yield. When 4 is treated with diethylaminosulfur trifluoride (DAST) under certain reaction conditions, a novel intramolecular second order allylic rearrange...

This study evaluates the performance of the newly developed high-resolution whole-body PET scanner ECAT EXACT HR+. The scanner consists of four rings of 72 bismuth germanate block detectors each, covering an axial field of view of 15.5 cm with a patient port of 56.2 cm. A single block detector is divided into an 8 x 8 matrix, giving a total of 32 r...

This study was performed to investigate the effect of the new chemotherapeutic agent gemcitabine on glucose transport and metabolism in prostate carcinoma in vitro and in vivo. After transplantation of rat prostate adenocarcinoma cells, dynamic PET measurements with fluorine-18-labeled 2-fluoro-2-deoxy-D-glucose (18FDG) were performed in 15 animals...

Using different tracers of tumor metabolism, the application of PET for monitoring gene therapy with the suicide gene herpes simplex virus thymidine kinase (HSVtk) is investigated in this in vitro study. Morris hepatoma cells were transfected with a retroviral vector bearing the HSVtk gene, and different clones were established by selection with th...

A new method for the efficient conversion of no-carrier-added [11C]carbon dioxide into [11C]carbon monoxide is described. [11C]Carbon dioxide produced by proton bombardment of ultra high purity nitrogen is pre-concentrated in a cryo trap and then passed through a quartz tube filled with a mesh of thin molybdenum wire heated to 850°C. [11C]Carbon di...

An efficient procedure for the preparation of oligonucleotides carrying a mono-N-substituted azamacrocycle and its radiolabeled complex with Cu-64 and Tc-99m is reported. The new derivatives are of potential interest for Positron Emission Tomography and Single Photon Emission Tomography.

Background: In spite of technical advances in conventional morphological imaging, these techniques cannot assess biological characteristics of a tumour. By contrast, positron emission tomography (PET) provides quantitative metabolic information of tumour and normal tissues. Although PET has demonstrated its value for diagnosis and follow-up of diff...

This study investigates the application of PET with specific substrates for the assessment of enzyme activity after transfer of the herpes simplex virus thymidine kinase (HSV-tk) gene. After transfection of a rat hepatoma cell line with a retroviral vector containing the HSV-tk gene, different clones were established by G418 selection. Uptake measu...

The management of patients who have malignant lymphomas requires functional methods to differentiate residual soft tissue masses. Positron emission tomography (PET) was performed in patients with histologically proven malignant lymphomas prior to the onset of second-line chemotherapy to examine tumor viability. Twenty patients (68 malignant lesions...

The management of patients who have malignant lymphomas requires functional methods to differentiate residual soft tissue masses. Positron emission tomography (PET) was performed in patients with histologically proven malignant lymphomas prior to the onset of second-line chemotherapy to examine tumor viability. Twenty patients (68 malignant lesions...

Several nucleoside analogues like 1-(β-D-glucopyranosyl)-5-fluorouracil 10, 1-(β-D-galactopyranosyl)-5-fluorouracil 11 and 1-(2-deoxy-β-D-glucopyranosyl)-5-fluorouracil 12 have been synthesized. From the corresponding 1-(2′,3′,4′,6′-tetra-O-acetyl-β-D-glycopyranosyl)-uracils 4, 5 and 6, the 18F labelled compounds 16, 17 and 18 have been prepared vi...

Positron emission tomography (PET) is a noninvasive functional method for the study of solid tumor perfusion, metabolism and interaction with different therapeutic agents. The aim of the study was the investigation of the metabolism of hepatocellular carcinomas (HCC) and the kinetics during a treatment with intratumoral ethanol by PET. The ongoing...

Hematopoietic growth factors (HGF) such as G-CSF and GM-CSF stimulate cell growth of the bone marrow and thereby mitigate the myelotoxic effect of chemotherapy. Using 18F-fluoro-2-deoxy-D-glucose (FDG) positron emission tomography (PET) for therapy response monitoring of patients with small-cell lung cancer, both an extension and an intensification...

The nonphysiological, nonracemic, branched-chain alpha-acetamido-aminoisobutyric acid was labeled with the carbon isotope 11C with the intention to use it in conjunction with positron emission tomography (PET) to measure the kinetics of amino acid transport in vivo. It was produced by the reaction of the novel 11C-precursor N-[1-11C]acetylpyridiniu...

We report an attractive approach for the preparation of [1-11C]acetate. The procedure involved the instantaneous hydrolysis of [1-11C]acetyl chloride back to [1-11C]acetic acid by simply trapping the volatile acid chloride in physiological saline. This delivered [1-11C]acetate immediately in pharmaceutical quality. An easy and quantitative gas phas...

Up to 4 h after treatment of human SW 707 colon carcinoma cells with the antineoplastic drug 4-amino-N-(2'-aminophenyl)-benzamide (GOE 1734, dinaline), the effects of tumour cell metabolism and proliferation were examined in vitro. Four tracers which can be labelled with isotopes suitable for positron emission tomography (PET) were used for this pu...

Genetically modified mammalian cells that express the cytosine deaminase (CD) gene are able to convert the nontoxic prodrug 5-fluorocytosine (5-FC) to the toxic metabolite 5-fluorouracil (5-FU). PET with 18F-5-FC may be used for in vivo measurement of CD activity in genetically modified tumors. A human glioblastoma cell line was stably transfected...

The bacterial enzyme cytosine deaminase (CD) catalyzes the conversion of 5-fluorocytosine (5-FC) to the lethal 5-fluorouracil (5-FU) and so provides a useful system for selective killing of gene-modified mammalian tumor cells. Cloning of the CD gene from Escherichia coli and expression in human tumor cell lines enabled these cells to convert 3H-lab...

Up to 4 h after treatment of human SW 707 colon carcinoma cells with the antineoplastic drug 4-amino-N-(2-aminophenyl)-benzamide (GOE 1734, dinaline), the effects of tumour cell metabolism and proliferation were examined in vitro. Four tracers which can be labelled with isotopes suitable for positron emission tomography (PET) were used for this pur...

A novel intramolecular vinylogous substitution of D-galactal (1) is described. The resulting 1,6-anhydro-2,3-dideoxy-β-D-threohex-2-enopyranose (4) can, after protection with various groups, easily be transformed into mono- and dihalocompounds (6), (9), (10), (11), (15), (16) and (17) either directly or via the the Cerny epoxides (12) and (14).

Background: Aim of the study was the biological characterization of melanoma metastases. Material and Methods: 27 patients with metastatic malignant melanoma (MM) were examined with PET and the radiotracers ¹⁸F-2- deoxy-D-glucose (FDG) and ¹⁵O-labeled water to determine metabolism and perfusion of the metastases. Results: The PET-FDG scans 60 min p...

N-Acetyl-leukotriene E4 has been identified as an endogenous, biologically less active cysteinyl leukotriene metabolite in rodents and humans. To evaluate the ratio of hepatobiliary to renal elimination of leukotrienes noninvasively by positron emission tomography (PET), we synthesized N-[11C]acetyl-leukotriene E4 by chemical N-acetylation of leuko...

Derivatives of alanine, α-[2-11C]aminoisobutyric acid 1a and α-(N-methyl)-[2-11C]aminoisobutyric acid 1b were prepared for the in-vivo study of amino acid transport phenomena by positron-emission-tomography (PET). Compounds 1a and 1b were obtained by a Zelinski-Stadnikoff variant of the Strecker α-amino acid synthesis from in-situ formed [11C]aceto...

Unsere Untersuchungen sollten zeigen, ob Interferon-a (IFNa) einen Einfluß auf die metabolische Aktivierung und die Pharmakokinetik von Dacarbazin (DTIC) in vitro und bei Patienten mit metastasierendem Melanom besitzt. Die Analyse von DTIC und dessen Metaboliten AIC im Plasma von Patienten erfolgte mittels Hochleistungsflüssig- keitschromatografie...

Rat prostate adenocarcinoma cells were used to evaluate different incubation procedures for the measurement of fluorodeoxyglucose (FDG) uptake and to measure the effects on chemotherapy. The cells were incubated for 10 or 60 min in media with different glucose concentrations. Furthermore, the cells were treated for 4 hr with different doses of gemc...

To determine the influence of tumor cell proliferation and changes in the genetic program in malignant cells on the fluorodeoxyglucose (FDG) uptake we performed PET studies in several animal tumors: spontaneous mammary fibroadenoma, chemically-induced mammary adenocarcinoma and Dunning prostate adenocarcinoma. The expression of the glucose transpor...

Two cell lines derived from a lung metastasis of a rat osteosarcoma were treated with cisplatin (CDDP) and two phosphonic acid compounds (AMDP, DADP), AMDP-treated cells showed a decrease in FDG uptake, CDDP and DADP resulted in an increase. A block in G2 or in S and G2 phase was seen after CDDP and AMDP treatment. The changes in the cell cycle fra...

Positron emission tomography (PET) was applied to evaluate therapeuticeffectsin patientswith advancedheadand neck cancer for use in monitoring therapy. In 18 patients with histologically proven head and neck cancer, PET studies with 330†" 440 MBq 18F-fluorodeoxyglucose(FDG)were performed prior to the first chemotherapeutic cycle with cisplatin an...

Fluorouracil (FU) is the most common cytostatic agent used for chemotherapy in patients with colorectal tumors. Fifty patients with 78 hepatic metastases from colorectal tumors were examined with positron emission tomography (PET) following intravenous infusion of 18F-FU. The uptake of the cytostatic agent was evaluated in normal liver parenchyma,...

Alkylation of ethyl 2-(2,2,5,5-tetramethyl-[1,2,5,]azadisilolidine-1-yl)propionate with [11C]CH3I afforded, following acid hydrolysis and chromatographic purification, the non-physiological α-[3-11C]aminoisobutyric acid within 40 min in yields of 5 - 15% (not corrected for decay) related to initially produced [11C]CH3I. Usually 1.2·109 Bq of the tr...

Positron emission tomography (PET) was applied to evaluate therapeutic effects in patients with advanced head and neck cancer for use in monitoring therapy. In 18 patients with histologically proven head and neck cancer, PET studies with 330-440 MBq 18F-fluorodeoxyglucose (FDG) were performed prior to the first chemotherapeutic cycle with cisplatin...

Die bisher nur schwer zugänglichen Dianhydropyranosen 1 und 2 können überraschend einfach und in guter Ausbeute in jeweils einem Schritt aus dem Pseudoglucalderivat 3 erhalten werden. Das verbrückte Glucosid 3 entsteht aus Glucal in einer für diesen Verbindungstyp neuartigen intramolekularen Ringschlußreaktion. RH.

Previously difficult to obtain, dianhydropyranoses 1 and 2 can now be synthesized from the pseudoglucal derivative 3 in one step with surprising ease and in good yields. The bridged glucoside 3 is prepared from glucal by an intramolecular ring-closure novel for this type of compound. R = H.(~)[GRAPHICS]

Alkylation of ethyl 2‐(2,2,5,5‐tetramethyl‐[1,2,5,]azadisilolidine‐1‐yl)propionate with [11C]CH3I afforded, following acid hydrolysis and chromatographic purification, the non‐physiological α‐[3‐11C]aminoisobutyric acid within 40 min in yields of 5 ‐ 15% (not corrected for decay) related to initially produced [11C]CH3I. Usually 1.2·109 Bq of the tr...

In order to quantify effects of an experimental chemotherapy, MCF7 cells were studied with 14C-fluorodeoxyglucose (FDG) and high-performance liquid chromatography (HPLC). Uptake measurements were performed 1 and 4 hr after the end of a therapy with hexadecylphosphocholine (HPC). A dose- and time-dependent increase of the FDG uptake after therapy wa...

Abstract5(S)‐Hydroxy‐6(R)‐(N‐[1‐11C]acetyl)cysteinyl‐7,9‐trans‐11,14‐cis‐eicosatetraenoic acid (N‐[1‐11C]acetyl leukotriene E4) was prepared by the reaction of leukotriene E4 and [1‐11C]acetyl chloride. The product was obtained with 1.3% yield, based on [1‐11C]acetyl chloride. The preparation required 50 min from the end of radioisotope production....

5(S)-Hydroxy-6(R)-(N-[1-C-11]acetyl)cysteinyl-7,9-trans-11,14-cis-eicosatetraenoic acid (N-[1-C-11]acetyl leukotriene E4) was prepared by the reaction of leukotriene E4 and [1-C-11]acetyl chloride. The product was obtained with 1.3% yield, based on [1-C-11]acetyl chloride. The preparation required 50 min from the end of radioisotope production. The...

The non-invasive diagnostic assessment of thoracic lesions has been greatly enhanced by the use of positron emission tomography with metabolic active radio-compounds such as fluor-18 labeled deoxyglucose. Four clinical fields of use were established: differential diagnostic evaluation of lesions (T-staging); classification of adenopathy (N-staging)...

Treatment of tri-O-acetyl-D-galactal with xenon difluoride at −20 to +5 0C in CFCl3 afforded, after hydrolysis, 2-deoxy-2-fluoro-D-galactose in a smooth and stereoselective reaction. Preparative HPLC on a cation exchange resin delivered the white, crystalline product in yields of 63%.

2-Deoxy-2-fluoro-D-galactose (dGalF), added to the medium of primary cultured rat hepatocytes, inhibited N-glycosylation of membrane (gp 120) and secretory glycoproteins (alpha 1-macroglobulin) in a concentration-dependent manner. Complete inhibition of N-glycosylation was achieved at concentrations of 1 mM and above. At identical concentrations, 2...

The quantitation of physiological functions by means of positron emission tomography (PET) requires radiolabelled metabolic substrates which contain a suitable positron emitting radionuclide. The number of positron emitting labels is limited, and only fluorine-18 and bromine -75 are suitable halogensfor PET studies in humane medicine. This short re...

The increasing number of different therapeutic protocols necessitates an early objective evaluation of therapy response. Depending on significant response to the ongoing therapy, the chosen protocol is continued, or alternative protocols are used. Current diagnostic imaging techniques, from conventional radiology to computed tomography and magnetic...

For the evaluation and individual planning of chemotherapy or head and neck tumors it is useful to obtain information about the tumor metabolism and its early changes during chemotherapy. Positron emission tomography (PET) with [18F]fluorodeoxyglucose (FDG) is a specific method that gives information about glucose uptake. These data can be used in...

The standard chemotherapeutic agent for the treatment of hepatic metastases from colorectal cancer is 5-fluorouracil (FU) [1]. Depending on both the selection process and the response criteria used, the reported response rates have varied from 8% to 82% [1]. Based on a literature survey, Kemeny reported that the average response rate for liver meta...

Forty-four patients with recurrent colorectal carcinoma were examined prior to a combination of conventional photon radiotherapy (40 Gy) and neutron therapy (10 Gy). Twenty-one of these underwent a PET examination after photon therapy and 12 also were studied after the end of combined therapy. CEA plasma levels were measured from blood samples take...

The uptake of laF-Deoxyglucose (FDG) was studied in vivo in relation to the proliferation rate of human head and neck tumors. Forty-two patients with histologically proven squa-mous-cell carcinoma of the head and neck and four patients with metastases of head and neck tumors were examined with PET and FDG prior to surgery. In 35 of these patients,...

The interaction of weakly acidic monosaccharides with a polystyrene sulphonate in the H+ form resulted in unexpected selectivity for epimeric aldohexoses, deoxyaldohexoses and deoxyfluoroaldohexoses. This led to a new application of high-performance chromatography. The separation is dominated solely by the electrostatic interaction between carbohyd...

The synthetic d ‐galactose analog 2‐deoxy‐2‐fluoro‐ d ‐galactose (dGalF) offers unique advantages for studies of the d ‐galactose pathway by non‐invasive techniques using ¹⁹ F‐NMR spectroscopy or positron emission from the ¹⁸ F‐labeled compound. The metabolism of 2‐deoxy‐2‐fluoro‐ d ‐galactose was studied in rodents using the unlabeled, the ¹⁸ F‐la...

The metabolism of 2-deoxy-2-fluoro-D-galactose (dGalF) was studied in rodents using HPLC, enzymatic methods, and 19F-NMR spectroscopy in vivo and in vitro. The liver took up the major part of the administered dose of the 14C-labeled D-galactose analog. This was confirmed in vivo by use of the 18F-labeled sugar (1.5 mCi/kg; 25 mumol/kg) and examinat...

Positron emission tomography (PET) was used in the follow-up of patients with colorectal malignancies to differentiate between recurrent colorectal tumor and scar. Patients were examined with oxygen-15-labeled water and with fluorine-18-labeled deoxyglucose (FDG). FDG was injected intravenously to assess tumor metabolism. The tracer concentration w...

Treatment of EL-4 lymphoma cells with tetradecanoylphorbol-acetate (TPA), a well-known activator of protein kinase C, induces the production of the T cell growth factor interleukin-2 (IL-2) and the expression of IL-2-specific mRNA within 4-8 h. This system is an ideal model for studies on the induction of a differentiated function in a homogeneous...

5-[18F]Fluorouracil was prepared by direct fluorination of uracil in acetic acid using [18F]F2 diluted in neon. The labelled product was obtained with a purity of ≥99% following preparative HPLC. Quality control consisted of two different and improved HPLC procedures combined with high resolution NMR spectroscopy for analyzing directly the HPLC elu...

The new 18F-labelled precursor 1-[18F]fluoro-2-pyridone was prepared by reacting [18F]F2 with 2-(trimethylsiloxy)pyridine. This compound has potential as an easy to use yet selective labelling reagent in preparations, where fluorine carrier may be tolerated. Pure (>92%) 1-[18F]fluoro-2-pyridone is obtained within 35 min from end of bombardment in y...

N-Fluoropyridinium triflate was labelled with 18F proceeding through N-trimethylsilylpyridinium triflate and [18F]F2 diluted to 1% in Ne. A typical experiment afforded this new fluorine-18 transfer reagent with up to 46% radiochemical yield. The specific activity of 18F-labelled N-fluoropyridinium triflate was determined by iodometric titration to...

A procedure has been developed that allows the separation of 2-deoxy-2-[18F]fluoro-D-glucose from 2-deoxy-2-[18F]fluoro-D-mannose employing selectively optimized ion-moderated partition chromatography. Both compounds can be obtained with a greater than 98% chemical and radiochemical purity in about one half-life of 18F. Both the alpha- and beta-ano...

11C-Suriclone was synthetised in a short time (30 minutes) with a high specific activity (750 mCi/ m̈Mol) for studies in man with the Positron Emission Tomography technic. The starting material was the N-demethylated product 35489 RP. The radioactive reagent was either 11C-formaldehyde or 11C-methyl iodide.

The use of diphosphorous tetraiodide for the preparation of [11C]methyl iodide from [11C]methanol has been investigated. This method offers several practical advantages over the established procedure using hydrogen iodide. [11C]Methyl iodide, produced by this new route, has been obtained in a radiochemical yield of 80–90% with a radiochemical purit...

1-11C-n-Butanol produced semiatomatically using a cyclotron was employed to investigate the whole-body distribution and kinetics of the label of this compound. Following the administration of 11C-butanol into the aorta of two dogs, more than 80% of the activity was cleared from the blood within 1 min. The activity distribution mirrored the cardiac...