A synthesis of olanzapine, 2-methyl-10-(4-methyl-1-piperazinyl)-4H-thieno[2,3-b][1,5]benzodiazepine was carried out, and the conditions for its tritium labeling were optimized, to get a tritium-labeled olanzapine preparation with molar radioactivity of 12 Ci/mmol.
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http://dx.doi.org/10.1007/s11171-005-0052-2 | DOI Listing |
Radiat Prot Dosimetry
November 2024
Laboratory of Radiological Disasters and Medical Science, International Research Institute of Disaster Science, Tohoku University, 519-1176 Aramaki-aza-Aoba, Aoba-ku, Sendai 980-0845, Japan.
This study investigated the induction of DNA double-strand breaks (DSBs) in the hTERT-immortalized normal human diploid epithelial cells (RPE1-hTERT) continuously exposed to 6000 Bq/ml of tritiated water (HTO) and organically bound tritium (OBT). The relationship of the DSBs induction with the intracellular amount as well as the localization of tritium was also examined. Tritium-labeled thymidine (3H-Thy) and palmitic acid (3H-PA) were used as OBT.
View Article and Find Full Text PDFArch Insect Biochem Physiol
November 2024
Biological Control of Insects Research Laboratory, Columbia, Missouri, USA.
Prostaglandin E (PGE) is an eicosanoid that mediates a range of physiological actions in vertebrates and invertebrates, including reproduction and immunity. The PGE receptor was identified and functionally assessed in two lepidopteran insects, Manduca sexta and Spodoptera exigua. However, its binding affinity to the receptor has not been reported.
View Article and Find Full Text PDFMolecules
August 2024
State Key Laboratory of Bioactive Substances and Function of Natural Medicine, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China.
With low background radiation, tritiate compounds exclusively emit intense beta particles without structural changes. This makes them a useful tool in the drug discovery arsenal. Thanks to the recent rapid progress in tritium chemistry, the preparation and analysis of tritium-labeled compounds are now much easier, simpler, and cheaper.
View Article and Find Full Text PDFBiol Pharm Bull
September 2024
Faculty of Pharmacy, Kanazawa University.
Eur J Med Chem
August 2024
Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai, 201203, China. Electronic address:
DNA methyltransferase 1 (DNMT1) is the primary enzyme responsible for maintaining DNA methylation patterns during cellular division, crucial for cancer development by suppressing tumor suppressor genes. In this study, we retained the phthalimide structure of N-phthaloyl-l-tryptophan (RG108) and substituted its indole ring with nitrogen-containing aromatic rings of varying sizes. We synthesized 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids and confirmed them as DNMT1 inhibitors through protein affinity testing, radiometric method using tritium labeled SAM, and MTT assay.
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