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/ISA | Acebutolol (2.4#) Practolol (>14.1#) | Labetalol (2.5#) Alprenolol (16.2#) |
| Inverse agonist | Metoprolol (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.