676494-58-9Relevant academic research and scientific papers
Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: Application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer
Mitch, Charles H.,Quimby, Steven J.,Diaz, Nuria,Pedregal, Concepcion,De La Torre, Marta G.,Jimenez, Alma,Shi, Qing,Canada, Emily J.,Kahl, Steven D.,Statnick, Michael A.,McKinzie, David L.,Benesh, Dana R.,Rash, Karen S.,Barth, Vanessa N.
, p. 8000 - 8012 (2011)
Arylphenylpyrrolidinylmethylphenoxybenzamides were found to have high affinity and selectivity for κ opioid receptors. On the basis of receptor binding assays in Chinese hamster ovary (CHO) cells expressing cloned human opioid receptors, (S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl) phenoxy)benzamide (25) had a Ki = 0.565 nM for κ opioid receptor binding while having a Ki = 35.8 nM for μ opioid receptors and a Ki = 211 nM for δ opioid receptor binding. Compound 25 was also a potent antagonist of κ opioid receptors when tested in vitro using a [35S]-guanosine 5′O-[3-thiotriphosphate] ([35S]GTP-γ-S) functional assay in CHO cells expressing cloned human opioid receptors. Compounds were also evaluated for potential use as receptor occupancy tracers. Tracer evaluation was done in vivo, using liquid chromatography-tandem mass spectrometry (LC/MS/MS) methods, precluding the need for radiolabeling. (S)-3-Chloro-4-(4-((2-(pyridine-3-yl)pyrrolidin-1-yl)methyl) phenoxy)benzamide (18) was found to have favorable properties for a tracer for receptor occupancy, including good specific versus nonspecific binding and good brain uptake.
Radiosynthesis of [11C]LY2795050 for Preclinical and Clinical PET Imaging Using Cu(II)-Mediated Cyanation
Yang, Lingyun,Brooks, Allen F.,Makaravage, Katarina J.,Zhang, Huibin,Sanford, Melanie S.,Scott, Peter J. H.,Shao, Xia
supporting information, p. 1274 - 1279 (2018/11/27)
Copper-mediated 11C-cyanation reactions have enabled the synthesis of PET radiotracers from a range of readily available precursors and avoid the need to use more toxic Pd catalysts. In this work we adapt our recently developed 11C-c
DIARYL ETHERS AS OPIOID RECEPTOR ANTAGONIST
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Page/Page column 150, (2008/06/13)
A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3', E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
