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This study examined the short term transfer of carbon-14 (C) in the common carp Cyprinus carpio under laboratory conditions. Various experiments were achieved in order to investigate direct or trophic transfer for 4 days, using waterborne C-labelled arginine or C-labelled food pellets respectively. Radiolabelled food was prepared with C-labelled arginine or glucose in order to test how transfer kinetics might vary with the biochemical form of C. Elimination experiments were achieved using fish fed for 5 days on radiolabelled food and then placed under starvation for 4 days. In all experiments, water, food and fish activities were monitored every day. Different fish fractions (whole body, muscle) were sampled in order to elucidate the role of muscle as a potential storage. Results suggested that direct water-to-fish absorption rate was 20% d per fish. Carps incorporated 14.3% of the absorbed C. Fish activity did not increase over days, due to a strong decrease in C concentration in the water (resulting from aquarium sorption). During trophic transfer experiments, food was entirely ingested and C sources rapidly assimilated. For either arginine or glucose, results suggested that 19-20% of ingested C was incorporated, yielding a significant increase in fish activity over days. No difference in mass-specific activity was observed among muscle and whole body. Total activity in the muscle represented 29%-32% of whole body activity, this proportion reflecting the contribution of muscle to whole body weight. During elimination experiments, results showed a significant decrease in whole body total activity and mass-specific activity with arginine. The decrease was not significant with glucose due to a great variability among fish. Results suggested that an essential amino-acid like arginine can be used as an energy source under starvation and that muscles can act as a storage for essential amino-acids.
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http://dx.doi.org/10.1016/j.jenvrad.2021.106585 | DOI Listing |
J Labelled Comp Radiopharm
July 2025
Chemistry Department, Gowan Novara, Novara, Italy.
The radiosynthesis of the systemic fungicide for oomycete disease control Benalaxyl-M and its two most relevant soil metabolites was developed from the versatile common [phenyl-U-C]N-(2,6-dimethylphenyl)-D-alanine methyl ester intermediate 4 by reaction with Meldrum's acid and subsequent hydrolysis of the ester group. The triflate of the methyl ester of (S)-lactic acid 6 employed in the synthesis of [phenyl-U-14C]N-(2,6-dimethylphenyl)-D-alanine methyl ester allows us an optimal use of the labelled [phenyl-U-14C]2,6-dimethylaniline. The greater reactivity of the triflate of the methyl ester of (S)-lactic acid compared to the analogous p-toluenesulfonate or methanesulfonate allows the reaction to occur at room temperature with higher enantiomeric purity and better yield.
View Article and Find Full Text PDFJ Labelled Comp Radiopharm
July 2025
Isotope Chemistry Laboratories, Almac Sciences Ltd., Almac House, Seagoe Industrial Estate, Craigavon, UK.
Three novel C-labelled isotopologues of the psychoactive agents psilocin, psilocybin and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT) were synthesised, all labelled at the 2-position of the indole. The syntheses involved incorporating the 3-dimethylaminoethyl substituent common to all three substances onto a 4- or 5-substituted indole intermediate via successive treatments with oxalyl chloride, dimethylamine and reduction with lithium aluminium hydride. Psilocybin-2-C with a specific activity of 234 μCi/mg exhibited limited stability, but a 5.
View Article and Find Full Text PDFJ Labelled Comp Radiopharm
June 2024
Therapeutics Discovery, Janssen Research and Development LLC, Spring House, Pennsylvania, USA.
Carbon-14 labeling synthesis of RORγt inhibitor JNJ-61803534 (1) was accomplished in four steps with the C14 label located at the thiazole-2-carboxamide carbon. The synthesis featured a highly efficient conversion of nitrile [C]-12 to ester [C]-17 under mild conditions via an imidate intermediate, overcoming the unsuccessful direct hydrolysis of nitrile 12 under either acidic or basic conditions. Since carbon-14 labeling via [C]-nitrile installation and subsequent conversion to [C]-carboxylic acid derivatives is a common labeling strategy, an efficient conversion of a nitrile to an ester under mild conditions could be of use for the future C14 labeling syntheses.
View Article and Find Full Text PDFJ Labelled Comp Radiopharm
June 2024
Corteva Agriscience, Indianapolis, Indiana, USA.
Rimsulfuron is a sulfonylurea herbicide that controls grass and broadleaf weeds in maize, potatoes, fruits, nuts, and other crops. It can also be used as a burndown herbicide to clear invasive weed species along roadsides and other nonagricultural land. Rimsulfuron acts as an acetolactase synthase (ALS) inhibitor, blocking the synthesis of essential amino acids required for plant growth.
View Article and Find Full Text PDFJ Labelled Comp Radiopharm
September 2023
The Radiosynthesis Laboratory, Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, Connecticut, USA.
(R)-2-(4-(Benzo[d]oxazol-2-yl)piperazin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (1) and (R)-2-(4-(4-chlorophenoxy)piperidin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (2) are two potent and selective inhibitors of phosphodiesterase type 4 (PDE4). In this manuscript, we report the detailed synthesis of these two compounds labeled with carbon 14 and with stable isotopes. The core (R)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide is common in both inhibitors.
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