Pm. Sher et al., CARBOXYL-PROMOTED ENHANCEMENT OF SELECTIVITY FOR THE BETA(3) ADRENERGIC-RECEPTOR - SELECTIVITY IS ENHANCED AT THE LEVEL OF RECEPTOR-BINDING, Medicinal chemistry research, 7(2), 1997, pp. 109-115
Four carboxyl-containing, selective beta(3) adrenergic agonists and th
eir ester or amide derivatives were evaluated for their ability to bin
d to human beta(1), beta(2), and beta(3) adrenergic receptors. Stimula
tory 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.