TABLE 1

Commonly used β-blockers and their relative β-adrenoceptor selectivity and partial agonist and inverse agonist properties

Cardioselective β1-blockers (relative selectivity of β1 versus β2)Nonselective β-blockers (relative selectivity of β1 versus β2)
Partial agonist/ISAAcebutolol (2.4#)
Practolol (>14.1#)
Labetalol (2.5#)
Alprenolol (16.2#)
Inverse agonistMetoprolol (2.3#, 6.0)
Atenolol (4.7#, 5.7)
Bisoprolol (13.5#, 19.6)
Nebivolol (40.6)
Carvedilol (4.5#)
Propranolol (8.3#)
Sotalol (12.0#)
Nadolol (23.4#)
Timolol (25.7#)

A relative selectivity ratio of 1 demonstrated equal activity at both β1- and β2-adrenoceptors. ISA: intrinsic sympathomimetic activity. #: according to Baker [26] using cell lines expressing human adrenoceptors; : according to Ladage et al. [49] in their review figure.