(±)-Befunolol is a blocking agent of β-adrenoceptor.

Befunolol, a β-adrenoceptor blocking agent, exhibits intrinsic sympathomimetic activities within the isolated right atria, trachea, and taenia caecum of guinea pigs, with intrinsic activities ranging from 0.22 to 0.28. The compound's pD2 values, obtained from these isolated organs, differ significantly from its pA2 values when antagonizing isoprenaline. This discrepancy suggests that Befunolol interacts with beta-adrenoceptors at potentially two distinct sites: one facilitating agonistic action and the other mediating competitive antagonistic action. The level of Befunolol's intrinsic activity might be indicative of its selectivity for these sites.