Search results for " Radioisotope"
showing 10 items of 246 documents
Spectroscopic, radiochemical, and theoretical studies of the Ga3+-N-2-hydroxyethyl piperazine-N'-2-ethanesulfonic acid (HEPES buffer) system: evidenc…
2013
Recent reports have claimed a superior performance of HEPES buffer in comparison to alternative buffer systems for 67/68 Ga labeling in aqueous media. In this paper we report spectroscopic (1H and 71 Ga NMR), radiochemical, mass spectrometry and theoretical modeling studies on the Ga3+/HEPES system (HEPES = N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid) performed with the aim of elucidating a potential contribution of HEPES in the 68/67 Ga radiolabeling process. Our results demonstrate that HEPES acts as a weakly but competitive chelator of Ga3+ and that this interaction depends on the relative Ga3+: HEPES concentration. A by-product formed in the labeling mixture has been identified …
A systematic comparison of kinetic modelling methods generating parametric maps for [11C]-(R)-PK11195
2006
[(11)C]-(R)-PK11195 is presently the most widely used radiotracer for the monitoring of microglia activity in the central nervous system (CNS). Microglia, the resident immune cells of the brain, play a critical role in acute and chronic diseases of the central nervous system and in host defence against neoplasia. The purpose of this investigation was to evaluate the reliability and sensitivity of five kinetic modelling methods for the formation of parametric maps from dynamic [(11)C]-(R)-PK11195 studies. The methods we tested were the simplified reference tissue model (SRTM), basis pursuit, a simple target-to-reference ratio, the Logan plot and a wavelet based Logan plot. For the reliabilit…
Gallium-68 and scandium-44 labelled radiotracers based on curcumin structure linked to bifunctional chelators: Synthesis and characterization of pote…
2019
Abstract Curcumin metal complexes showed widespread applications in medicine and can be exploited as a lead structure for developing new tracers for nuclear medicine application. Herein, the synthesis, chemical characterization and radiolabelling with gallium-68 and scandium-44 of two new targeting vectors based on curcumin scaffolds and linked to the chelators 1,4,7-triazacyclononane,1-glutaric acid-4,7-acetic acid (NODAGA) and 1,4-bis(carboxymethyl)-6-[bis(carboxymethyl)]amino-6-methylperhydro-1,4-diazepine (AAZTA) are reported. Synthesis of the precursors could be achieved with a 13% and 11% yield and radiolabelling generally afforded rapid incorporation under mild conditions (>95%). Sta…
A convenient chemo-enzymatic synthesis and 18F-labelling of both enantiomers of trans-1-toluenesulfonyloxymethyl-2-fluoromethyl-cyclopropane
2008
The present report is concerned with a stereoselective, reliable route to trans-1,2-disubstituted cyclopropanes and in particular to (S,S)-1-tosyloxymethyl-2-fluoromethyl-cyclopropane (1) and (R,R)-1-tosyloxymethyl-2-fluoromethyl-cyclopropane (ent-1) as conformationally restricted, terminally fluorinated C4-building blocks for medicinal chemistry. The enzymatic kinetic resolution based synthesis of 1 and ent-1 utilises inexpensive, commercially available starting materials. It is based on enantiomeric resolution of rac-cyclopropane carboxylic esters using esterase from Streptomyces diastatochromogenes. Both enantiomers of 1 were prepared selectively in high overall yield over nine steps, st…
Induction of DNA single-strand breaks by 131I and 99mTc in human mononuclear blood cells in vitro and extrapolation to the in vivo situation.
2000
The radionuclides (131)I and (99m)Tc are frequently used for therapy of benign and malignant thyroid disease ((131)I) and for diagnosis of thyroid and other diseases ((99m)Tc). However, the levels of DNA single-strand breaks (SSBs) induced in cells of patients after administration of (131)I and (99m)Tc are not known. In this study, we measured the number of SSBs per cell induced by (131)I and (99m)Tc in vitro, extrapolated the results to the clinical situation, and assessed their biological relevance by comparing levels of SSBs induced after therapeutic administration of (131)I and (99m)Tc to those induced by endogenous processes or by occupational exposure to genotoxic substances. A linear…
In vivo comparison of DOTA based 68Ga-labelled bisphosphonates for bone imaging in non-tumour models.
2013
Bone metastases are a class of cancerous metastases that result from the invasion of a tumor into bone. The solid mass which forms inside the bone is often associated with a constant dull ache and severe spikes in pain, which greatly reduce the quality of life of the patient. Numerous (99m)Tc-labeled bisphosphonate functionalised complexes are well established tracers for bone metastases imaging. The objective of this research was to evaluate the pharmacokinetics and behaviour of three DOTA based bisphosphonate functionalised ligands (BPAMD, BPAPD and BPPED), using both (68)Ga μ-PET in vivo imaging and ex vivo biodistribution studies in healthy Wistar rats. The compounds were labelled with …
A comparative investigation of DNA adducts, DNA strand breaks and gene mutations induced by benzo[a]pyrene and (+/-)-anti-benzo[a]pyrene-7,8-diol 9,1…
1997
Abstract Genotoxic effects of benzo[ a ]pyrene (BP) and its reactive metabolites (±)- anti -benzo[ a ]pyrene-7,8-diol 9,10-oxide ((±)- anti -BPDE) were comparatively investigated in vitro with the permanent human fibroblast cell line MRC5CV1. Induced DNA adducts were measured by 32 P-postlabeling, DNA strand breakage was determined by the comet assay and the HPRT gene mutation test was used to detect cytotoxicity and mutagenicity. Treatment of MRC5CV1 cells with S9 mix-activated BP or with (±)- anti -BPDE resulted in a concentration-dependent increase in DNA adducts and strand breaks. Genotoxic effects of BP and (±)- anti- BPDE were detected by 32 P-postlabeling and the comet assay with sim…
Design of a power conditioning unit for a Stirling generator in space applications
2012
The Free-Piston Stirling Generator (FPSG) is a thermal to electrical energy conversion system, based upon the thermal engine of the same name. Intensive research concerning the feasibility of the engine for its application in deep space and planetary missions has been conducted, primarily due to the potential increase in efficiency (−30%) over the currently used Radio-isotope Generators (RTGs). On the other hand, less attention has been paid to the power conditioning requirements and alternatives. The present work has investigated on the dynamics governing the FPSGs in order to assess the design requirements for the subsequent power-conditioning unit (PCU). Thereafter, two alternatives of A…
A model for the formation and degradation of bound residues of the herbicide 14C-isoproturon in soil
1999
Abstract The humic monomer catechol was reacted with 14 C-isoproturon and some of its metabolites, including 14 C-4-isopropylaniline, in aqueous solution under a stream of oxygen. Only in the case of 14 C-4-isopropylaniline, incorporation in oligomers, in fulvic acid-like polymers, and in humic acid-like polymers was observed. The main oligomer was identified by mass spectrometry as 4,5-bis-(4-isopropylphenylamino)-3,5-cyclohexadiene-1,2-dione. Oligomers and polymers containing bound 14 C-4-isopropylaniline were subjected to biodegradation studies in a loamy agricultural soil during 55 days by quantifying 14 CO 2 evolved. In all cases, significant mineralization rates could be determined, w…
A laboratory study of the mineralization and binding of 14C-labeled herbicide rimsulfuron in a rendzina soil
1999
Abstract The fate of pyrimidine-2- 14 C-rimsulfuron in a rendzina soil was investigated using a laboratory microcosm approach. Measurement of CO 2 evolution suggested that rimsulfuron applied at 5 times the recommended dose did not affect soil respiration. Under abiotic conditions, no mineralization of 14 C-rimsulfuron into 14 C-CO 2 occured and under biotic ones it was very low reaching 0.75 % of the applied 14 C-rimsulfuron after 246 days of incubation. The analysis of data showed that a three-half order model provided the best fit for the mineralization curve. Extractable 14 C-residues decreased over time to 70 – 80% of the applied 14 C-rimsulfuron at the end of the incubation. After 246…