Vibegron shows high selectivity and potent agonist activity for β3-adrenoceptors, irrespective of receptor density.

ABSTRACT: β3-Adrenoceptor (AR) agonists are used to treat patients with an overactive bladder (OAB). Clinical proof-of-concept data have been obtained for the β3-AR agonists vibegron, mirabegron, solabegron, and ritobegron; however, the selectivities of these agents have not been compared directly under the same experimental conditions. Moreover, the bladders of some patients express lower β3-AR densities than those of healthy individuals, and the β3-AR density might be expected to affect agonist activity. This study assessed the β3-AR selectivities of four β3-AR agonists and examined the effects of β-AR density on their pharmacological profiles. Functional cellular assays were performed using Chinese hamster ovary-K1 cells expressing three human β-AR subtypes transfected with different amounts of p

SUBMITTER: Yamamoto S 

PROVIDER: S-EPMC10473532 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature