Journal of Labelled Compounds and Radiopharmaceuticals This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Practical approaches to labelling terminal alkynes with deuterium
Terminally deuterated alkynes may be prepared by base-catalysed isotope exchange with deuterium oxide, using sodium hydroxide, calcium oxide, or N,N,N,N-tetramethylguanidine as catalysts. Silver perchlorate is a more suitable catalyst when labelling alkynes which are sensitive to base, or which contain functionalities which would lead to base-catalysed labelling elsewhere in the molecule. The silver-catalysed procedure is regiospecific and gives excellent yields and high deuterium abundances. Base catalysed exchange with sodium hydroxide, calcium oxide orN,N,N,N-tetramethylguanidine in deuterium oxide is a viable procedure...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 3, 2022 Category: Biochemistry Authors: Melanie Y. T. Chan, Arbab Anwar, William J. S. Lockley Tags: RESEARCH ARTICLE Source Type: research

Synthesis of Carbon ‐14 and Stable Isotope Labeled Censavudine
Censavudine is a nucleoside reverse transcriptase inhibitor (NRTI) explored clinically by Bristol Myers Squibb for the treatment of human immunodeficiency virus-1 (HIV-1). As part of the development process, a carbon-14 labeled analog was synthesized for use in a human absorption, distribution, metabolism, and excretion (ADME) study. A stable isotope labeled analog was also synthesized for use as a mass spectrum internal standard in bioanalytical assays to accurately quantify the concentration of the drug in biological samples. Carbon-14 labeled Censavudine was synthesized in ten steps in a 9% overall yield from carbon-14 ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 2, 2022 Category: Biochemistry Authors: Richard C. Burrell, Samuel J. Bonacorsi, Adrian Ortiz, Tamas Benkovics, Zhongping Shi Tags: RESEARCH ARTICLE Source Type: research

Practical approaches to labelling terminal alkynes with deuterium
Base catalysed exchange with sodium hydroxide, calcium oxide or N,N,N,N-tetramethylguanidine in deuterium oxide is a viable procedure for the preparation of terminally deuterated alkynes for those alkynes stable to strong base. The use of silver perchlorate as a catalyst is an alternative practical option when labelling alkynes which are sensitive to base or contain functionalities which would lead to labelling elsewhere in the molecule. Labelling with this catalyst takes place smoothly at ambient temperature in a mixture of N,N-dimethylformamide and deuterium oxide. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 27, 2022 Category: Biochemistry Authors: Melanie Y. T. Chan, Arbab Anwar, William J. S. Lockley Tags: RESEARCH ARTICLE Source Type: research

Radioiodination of balsalazide, bioevaluation, and characterization as a highly selective radiotracer for imaging of ulcerative colitis in mice
This work focuses on tracking ulcerative colitis imaging in mice using [125/131I]balsalazide radiotracer to give high uptake of 75 ±1.90 percent injected dose/g organ (ID/g) confirmed the suitability of [131I]balsalazide as a novel radiotracer for ulcerative colitis imaging in mice. This work focuses on tracking ulcerative colitis in mice. High labeling yield and radiochemical purity were achieved for the formation of a [125/131I]balsalazide radiotracer at optimum conditions of oxidizing agent content (chloramines-T [Ch-T], 75  μg), substrate amount (100 μg), pH of reaction mixture (6), reaction time (30 min), and...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 18, 2022 Category: Biochemistry Authors: M.H. Sanad, Nermien M. Gomaa, Nermeen M. El Bakary, Ismail T. Ibrahim, Ayman Massoud Tags: RESEARCH ARTICLE Source Type: research

Synthesis and automated fluorine ‐18 radiolabeling of new PSMA‐617 derivatives with a CuAAC radiosynthetic approach
This paper focuses on the introduction in mild condition of fluorine-18 via a “click chemistry” copper-catalyzed azide-alkyne cycloaddition (CuAAC) radiosynthetic route. An alkyne derivative of PSMA-617, currently one of the most interesting target in prostate cancer imaging and therapy, was synthetized and radiolabelled with fluorine-18. The whole radiosynthetic procedur e was fully automated, and the final product was obtained in radiochemical good yield and purity, and proved to be stable in human plasma up to 4 h. In the last decade, the development of new radiopharmaceuticals for the imaging and therapy of prostat...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 11, 2022 Category: Biochemistry Authors: Marco N. Iannone, Stefano Stucchi, Elia A. Turolla, Chiara Beretta, Samuele Ciceri, Clizia Chinello, Lisa Pagani, Sergio Todde, Patrizia Ferraboschi Tags: RESEARCH ARTICLE Source Type: research

Initial evaluation of 99mTc ‐labeled anti‐carcinoembryonic antigen single‐chain fragment variable for micro‐single‐photon emission computed tomography imaging in mice with colorectal cancer
In this study, we report the production and radiolabeling of a novel anti-CEA single-chain fragment variable (scFv-96NRT, concentration for 50% of maximal effect 46  ng/ml), and evaluation of [99mTc]Tc-scFv-96NRT in non-invasive detection of CEA expression. [99mTc]Tc-scFv-96NRT was synthesized by one step reduction in labeling yield of>95% with radiochemical purity of>98% and molar activity of 10 –11 GBq/μmol. [99mTc]Tc-scFv-96NRT showed high stability in 0.01 M phosphate-buffered saline (PBS) and 5% human serum albumin (HSA). It exhibited elevated uptake in CEA over-expressing cells. Biodistribution studies i...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 10, 2022 Category: Biochemistry Authors: Xue Qin, Xiangxi Meng, Yao Xiong, Xiaoyi Guo, Yanan Ren, Li Wen, Qian Zhang, Hua Zhu, Zhi Yang Tags: RESEARCH ARTICLE Source Type: research

Exploring the enzyme ‐catalyzed synthesis of isotope labeled cyclopropanes
In this study, the use of enzyme-catalysis for the synthesis of labeled cyclopropanes was investigated. Two readily-available enzymes, a modified CYP450-enzyme and a modifiedAeropyrum pernic protoglobin, were investigated for the cyclopropanation of a variety of substituted styrenes. For this biocatalytic transformation, the enzymes required the use of ethyl diazoacetate. Due to the highly energetic nature of this molecule, alternatives were investigated. The final optimized cyclopropanation was successfully demonstrated usingn-hexyl diazoacetate, resulting in moderate to high enantiomeric excess. The optimized procedure w...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 7, 2022 Category: Biochemistry Authors: Malvika Sardana, Kim S. M ühlfenzl, Sylvia T. M. Wenker, Christian Åkesson, Martin A. Hayes, Charles S. Elmore, Subhash Pithani Tags: RESEARCH ARTICLE Source Type: research

Radioiodination of balsalazide, bioevaluation and characterization as a highly selective radiotracer for imaging of ulcerative colitis in mice.
This work focuses on tracking stomach ulcerative colitis in mice. High labeling yield and radiochemical purity were achieved for the formation of a [125/131I]balsalazide radiotracer at optimum conditions of oxidizing agent content (chloramines-T (Ch-T), 75 μg), substrate amount (100 μg), pH of reaction mixture (6), reaction time (30 min) and temperature (37oC), using radioactive iodine-125 (200-450 MBq). The radiolabeled compound, [125/131I]balsalazide, was stablein serum and saline solutionduring 24 hours. Balsalazide is acting as a peroxisome proliferator-activated receptors (PPAR γ). Biodistribution studies were carr...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 5, 2022 Category: Biochemistry Authors: M. H. Sanad, Nermien M. Gomaa, Nermeen M. El Bakary, Ismail T. Ibrahim, Ayman Massoud Tags: RESEARCH ARTICLE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 4, 2022 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Tritium hydrogen ‐isotope exchange with electron‐poor tertiary benzenesulfonamide moiety; application in late‐stage labeling of T0901317
Described is a late-stage tritium labeling of T0901317 using an HIE strategy in the electron-poor substrate lacking a goodortho-directing group for C ─H activation. Homogeneous catalysis with a Kerr-type catalyst provided [3H]T0901317 with SA of 10.8 Ci/mmol. Unprecedented translation issue of deuterium into tritium experiment during heterogeneous catalysis was observed, whereby efficient deuterium labeling conditions using Ir-black provided reasonable 0.72 D-enrichment of T0901317 but turned out to be ineffective when repeated under similar conditions in tritium experiments. The multifunctional radioligand [3H]T0901317 ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 4, 2022 Category: Biochemistry Authors: Tian Yongsong, B řetislav Brož, František Tureček, Aleš Marek Tags: RESEARCH ARTICLE Source Type: research

Initial evaluation of 99mTc ‐labeled anti‐CEA scFv for micro‐SPECT imaging in mice with colorectal cancer
In this study, we report the production and radiolabeling of a novel anti-CEA single-chain fragment variable (scFv-96NRT, concentration for 50% of maximal effect 46 ng/mL), and evaluation of [99mTc]Tc-scFv-96NRT in non-invasive detection of CEA expression. [99mTc]Tc-scFv-96NRT was synthesized by one step reduction in labeling yield of> 95% with radiochemical purity of> 98% and molar activity of 10-11 GBq/ μmol. [99mTc]Tc-scFv-96NRT showed high stability in 0.01 M phosphate buffered saline (PBS), and 5% human serum albumin (HSA). It exhibited elevated uptake in CEA over-expressing cells. Bio-distribution studies in B...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 30, 2021 Category: Biochemistry Authors: Xue Qin, Xiangxi Meng, Yao Xiong, Xiaoyi Guo, Yanan Ren, Li Wen, Qian Zhang, Hua Zhu, Zhi Yang Tags: RESEARCH ARTICLE Source Type: research

Synthesis and automated fluorine ‐18 radiolabeling of new PSMA‐617 derivatives with a CuAAC radiosynthetic approach
(Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 29, 2021 Category: Biochemistry Authors: M. N. Iannone, S. Stucchi, E. A. Turolla, C. Beretta, S. Ciceri, C. Chinello, L. Pagani, S. Todde, P. Ferraboschi Tags: RESEARCH ARTICLE Source Type: research