Tritium HIE with electron ‐poor tertiary benzenesulfonamide moiety; application in late‐stage labeling of T0901317
The multi-functional radioligand [3H]T0901317 ([3H]1) has been employed as a powerful autoradiographic tool to target several receptors, such as liver X, farnesoid X and retinoic acid-related orphan receptor alpha and gamma subtypes at nanomolar concentrations. Although [3H]1 is commercially available and its synthesis via tritiodebromination has been reported, the market price of this radioligand and the laborious synthesis of corresponding bromo-intermediate potentially preclude its widespread use in biochemical, pharmacological and pathological studies in research lab settings. We exploit recent reports on hydrogen-isot...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 28, 2021 Category: Biochemistry Authors: Yongsong Tian, B řetislav Brož, František Tureček, Aleš Marek 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 - December 3, 2021 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Radiolabeling and brain penetration of [11C]VU0071063, a ligand of type 1 sulfonylurea receptors for positron emission tomography imaging
Automated isotopic carbon-11 radiolabeling of SURI ligand VU0071063 was successfully developed to demonstrate in vivo the brain penetration of this tracer in healthy rats using PET imaging. Sulfonylurea receptor 1 (SUR1) overexpression in the central nervous system is a potential biomarker for positron emission tomography (PET) imaging of brain damage and recovery. VU0071063, a selective ligand of SUR1 able to cross the blood –brain barrier, was isotopically radiolabeled with carbon-11 from a desmethyl precursor obtained quantitatively in one step. Ready-to-inject [11C]VU0071063 was obtained in 18 ± 2% radiochemical...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 1, 2021 Category: Biochemistry Authors: Fabien Caill é, Wadad Saba, Sébastien Goutal, Louise Breuil, Bertrand Kuhnast, Nicolas Tournier Tags: RESEARCH ARTICLE Source Type: research