Selective A₃ Adenosine Receptor Antagonist Radioligand for Human and Rodent Species.

ABSTRACT: The A₃ adenosine receptor (A₃AR) is a target for pain, ischemia, and inflammatory disease therapy. Among the ligand tools available are selective agonists and antagonists, including radioligands, but most high-affinity non-nucleoside antagonists are limited in selectivity to primate species. We have explored the structure-activity relationship of a previously reported A₃AR antagonist DPTN 9 (N-[4-(3,5-dimethylphenyl)-5-(4-pyridyl)-1,3-thiazol-2-yl]nicotinamide) for radiolabeling, including 3-halo derivatives (3-iodo, MRS7907), and characterized 9 as a high -affinity radioligand [³H]MRS7799. A₃AR K _d values were (nM): 0.55 (human), 3.74 (mouse), and 2.80 (rat). An extended methyl acrylate (MRS8074,

SUBMITTER: Suresh RR 

PROVIDER: S-EPMC9014498 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature