Search results for "Carbon Radioisotopes"

Synthesis and PET studies of [11C-cyano]letrozole (Femara®), an aromatase inhibitor drug

2009

Abstract Introduction Aromatase, a member of the cytochrome P 450 family, converts androgens such as androstenedione and testosterone into estrone and estradiol, respectively. Letrozole (1-[bis-(4-cyanophenyl)methyl]-1 H -1,2,4-triazole; Femara) is a high-affinity aromatase inhibitor ( K i =11.5 nM) that has Food and Drug Administration approval for breast cancer treatment. Here we report the synthesis of carbon-11-labeled letrozole and its assessment as a radiotracer for brain aromatase in the baboon. Methods Letrozole and its precursor (4-[(4-bromophenyl)-1 H -1,2,4-triazol-1-ylmethyl]benzonitrile) were prepared in a two-step synthesis from 4-cyanobenzyl bromide and 4-bromobenzyl bromide,…

Response of Chinese Hamster V79 Multicellular Spheroids Exposed to High-Energy Carbon Ions

2004

Chinese hamster V79-379A spheroids 200 +/- 30 microm (+/- SD) in diameter were irradiated in agitated medium in different oxygen atmospheres with (1) 227 MeV/nucleon (12)C(+6) ions (plateau region) to model tissue in the entrance channel during therapy, (2) carbon ions in the extended Bragg peak modeling tissue in the target volume, or (3) X rays as a reference modality. Cell survival curves were similar for modes (1) and (3), indicating the absence of a contact effect and the presence of a pronounced oxygen effect with oxygen enhancement ratios (OERs) of 2.8 and 2.9, respectively. In contrast, the oxygen effect was substantially smaller in mode (2) with an OER of 1.4. Under normal or restr…

Effect of L-Histidine on the Survival of a T-Strain of Mycoplasma

1975

The addition of L-histidine to the growth medium prolongs the stationary phase and the survival of a T-strain of mycoplasma. Results of an experiment performed with 14 C-labeled urea demonstrate that the action of L-histidine is based on the retardation of the rise of pH.

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…

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…

An ethoxylated surfactant enhances the penetration of the sulfated laminarin through leaf cuticle and stomata, leading to increased induced resistanc…

2016

International audience; Some β-1,3-glucans and particularly sulfated laminarin (PS3) are known as resistance inducers (RIs) in grapevine against the downy mildew. However, their efficacy in vineyard is still often too low, which might be caused by a limited penetration through the leaf cuticle following spray application. We used (14) C-sucrose uptake experiments with grapevine leaves in order to select a surfactant as saccharide penetration enhancer. Our results showed that though sucrose foliar uptake was low, it was strongly enhanced by Dehscofix CO125 (DE), a highly ethoxylated surfactant. Fluorescent saccharides were then produced and laser scanning microscopy was used to analyze their…

Evidence of chloroethylene oxide being the reactive metabolite of vinyl chloride towards DNA: comparative studies with 2,2′ -dichloro-diethylether

1983

The roles of chloroethylene oxide (CEO) and chloroacetaldehyde (CAA) in carcinogenicity of vinyl chloride (VC) have been studied by comparing biological effects of VC exposure with those of 2,2'-dichlorodiethylether (bis(chloroethyl)ether, BCEE) as a metabolic precursor of CAA. Biological end-points investigated were covalent protein binding, nucleic acid (RNA and DNA) alkylation and the potency of the two chemicals to induce preneoplastic ATPase-deficient foci in rat liver. After exposure of rats to [1-14C]BCEE, BCEE derived radioactivity was bound to liver proteins. Analysis of hydrolysates of liver RNA and DNA gave no indication for the formation of either 7-N-(2-oxoethyl)guanine, 1,N6-e…

The DAT ligand [(18)F]PR17.MZ mirrors the in vivo pharmacokinetic profile of [(11)C]cocaine with significantly improved monoamine transporter selecti…

2010

The 13C urea breath test in the diagnosis of Helicobacter pylori infection

1999

Summary The urea breath test (UBT) is one of the most important non-invasive methods for detecting Helicobacter pylori infection. The test exploits the hydrolysis of orally administered urea by the enzyme urease, which H pylori produces in large quantities. Urea is hydrolysed to ammonia and carbon dioxide, which diVuses into the blood and is excreted by the lungs. Isotopically labelled CO2 can be detected in breath using various methods. Labelling urea with 13 C is becoming increasingly popular because this non-radioactive isotope is innocuous and can be safely used in children and women of childbearing age. Breath samples can also be sent by post or courier to remote analysis centres. The …