Celtarys Research Adenosine A3 Receptor fluorescent ligand as a new tool for the study of non-orthosteric interactions

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The group led by Dr. Eddy Sotelo at the University of Santiago de Compostela, in collaboration with the Uppsala University, has published a new article exploring non-orthosteric interactions of Adenosine A3 Receptor antagonists.

Among other research tools, the authors have use one of our potent and highly selective proprietary fluorescent ligands, CELT-228. CELT-228 shows a high affinity for Adenosine A3 Receptor, with a Ki of 57,2 nM and a high selectivity for this receptor subtype over the other receptors of its family, Adenosine A1 Receptor, Adenosine A2A Receptor and Adenosine A2B Receptor.

The paper shows a library of potent and highly A3AR selective pyrimidine- based compounds assembled through an efficient and succinct synthetic approach, which retain the A3AR potent and selective profile while improving the solubility of the original scaffold. The obtained results pave the way to explore newly functionalized A3AR ligands, including covalent drugs and molecular probes for diagnostic and delivery purposes.

See full article: https://pubs.acs.org/doi/10.1021/acsmedchemlett.1c00598