Table 2

Relative efficacies of TMQ isomers at β-adrenoceptor subtypes expressed in CHO cells

Compoundβ1-Adrenoceptor Fractional Receptor Occupancy2-aer2-bβ2-Adrenoceptor Fractional Receptor Occupancy2-aer2-bβ3-Adrenoceptor Fractional Receptor Occupancy2-aer2-b
(−)-Isoproterenol0.1310.2610.211
(±)-Trimetoquinol0.240.54n.d.2-c n.d.2-c 0.063.42
(+)-Trimetoquinol1.680.085.610.056.10.03
(−)-Trimetoquinol0.640.206.210.040.038.2
  • 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.