Carboxyl-promoted enhancement of selectivity for the beta(3) adrenergic receptor. Selectivity is enhanced at the level of receptor binding

Four carboxyl-containing, selective beta(3) adrenergic agonists and their ester or amide derivatives were evaluated for their ability to bind to human beta(1), beta(2), and beta(3) adrenergic receptors. Stimulatory effects on the beta(3) adrenergic receptor were also measured. We conclude that carboxyl-derived beta(3) functional selectivity Likely results, at least in part, from the effect of the carboxyl on binding selectivity.