Fluorescent H₂ Receptor Squaramide-Type Antagonists: Synthesis, Characterization, and Applications.

ABSTRACT: Fluorescence labeled ligands have been gaining importance as molecular tools, enabling receptor-ligand-binding studies by various fluorescence-based techniques. Aiming at red-emitting fluorescent ligands for the hH₂R, a series of squaramides labeled with pyridinium or cyanine fluorophores (19-27) was synthesized and characterized. The highest hH₂R affinities in radioligand competition binding assays were obtained in the case of pyridinium labeled antagonists 19-21 (pK _i: 7.71-7.76) and cyanine labeled antagonists 23 and 25 (pK _i: 7.67, 7.11). These fluorescent ligands proved to be useful tools for binding studies (saturation and competition binding as well as kinetic experiments), using conf

SUBMITTER: Biselli S 

PROVIDER: S-EPMC7429974 | biostudies-literature | 2020 Aug

REPOSITORIES: biostudies-literature