Compound | β1-Adrenoceptor Fractional Receptor Occupancy2-a | er2-b | β2-Adrenoceptor Fractional Receptor Occupancy2-a | er2-b | β3-Adrenoceptor Fractional Receptor Occupancy2-a | er2-b |
---|---|---|---|---|---|---|
(−)-Isoproterenol | 0.13 | 1 | 0.26 | 1 | 0.21 | 1 |
(±)-Trimetoquinol | 0.24 | 0.54 | n.d.2-c | n.d.2-c | 0.06 | 3.42 |
(+)-Trimetoquinol | 1.68 | 0.08 | 5.61 | 0.05 | 6.1 | 0.03 |
(−)-Trimetoquinol | 0.64 | 0.20 | 6.21 | 0.04 | 0.03 | 8.2 |
↵2-a Fractional receptor occupancy, fraction of the total population of receptors occupied by a drug to elicit a response equivalent to half-maximal response to (−)-isoproterenol calculated by the method of Furchgott and Bursztyn (1967).
↵2-b er, efficacy of drug relative to (−)-isoproterenol calculated as the ratio of fractional receptor occupancy of drug to fractional receptor occupancy of (−)-isoproterenol.
↵2-c n.d., not determined.