TABLE 1

Effect of β-AR agonists on cAMP accumulation in CHO cells expressing human β-ARs

Values represent the mean EC50 (in nanomolar), 95% CL (in brackets), and I.A. (in parentheses), respectively, of three to six preparations.

Compound
β-Adrenergic Activity
Selectivity
β1-AR
β2-AR
β3-AR
β1/β3
 β2/β3
Isoproterenol 11.1 [6.1-18.0] (1)a 1.8 [0.9-3.0] (1) 56.5 [27.7-107] (1) 0.20 0.03
YM178 >10,000b (0.1) >10,000b (0.1) 22.4 [12.6-36.3] (0.8) >446 >446
BRL37344 12,900 [10,000-18,900] (0.5) 360 [189-771] (0.7) 457 [386-544] (0.6) 28.2 0.79
CL316,243
>10,000b (0)
>10,000b (0.1)
4,430 [3250-6040] (0.5)
>2.3
>2.3

  • ↵ a I.A., value 1 corresponds to the I.A. equivalent of isoproterenol.

  • ↵b Could not be calculated because of low I.A.