Background:

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

A β-adrenoceptor blocking agent, Befunolol, is found to has intrinsic sympathomimetic activities in isolated right atria, trachea and taenia caecum of guinea pig (intrinsic activities are 0.22-0.28). The pD2-values of Befunolol estimated in the isolated organs are significantly different from its pA2-values against isoprenaline. Befunolol interacts with the beta-adrenoceptor where there may be two different sites: one site for agonistic action and the other for competitive antagonistic action. The intrinsic activity of Befunolol may be equal to its selectivity for both the sites[1].

[1]. Takayanagi I, et al. A beta-adrenoceptor blocking agent, befunolol as a partial agonist in isolated organs. Gen Pharmacol. 1985;16(3):265-7.