Optical control of the β₂-adrenergic receptor with opto-prop-2: A cis-active azobenzene analog of propranolol.

ABSTRACT: In this study, we synthesized and evaluated new photoswitchable ligands for the beta-adrenergic receptors β₁-AR and β₂-AR, applying an azologization strategy to the first-generation beta-blocker propranolol. The resulting compounds (Opto-prop-1, -2, -3) have good photochemical properties with high levels of light-induced trans-cis isomerization (>94%) and good thermal stability (t _1/2 > 10 days) of the resulting cis-isomer in an aqueous buffer. Upon illumination with 360-nm light to PSS _cis , large differences in binding affinities were observed for photoswitchable compounds at β₁-AR as well as β₂-AR. Notably, Opto-prop-2 (VUF17062) showed one of the largest optical shifts in binding affini

SUBMITTER: Bosma R 

PROVIDER: S-EPMC9436767 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature