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. 2014 Feb 8;5(4):416–421. doi: 10.1021/ml4005232

Table 1. Potency and Intrinsic Activity at the Human β2AR.

graphic file with name ml-2013-005232_0008.jpg

compd no. R1 R2 R3 β2 potency pEC50a IAb
1 H nBu phenethyl 8.8 0.9
2 H -(CH2)2NEt2 phenethyl 8.1 0.9
3 OH -(CH2)2NEt2 phenethyl 8.4 1.0
4 OH -(CH2)2NEt2 3-chlorophenethyl 8.4 0.9
5 H -(CH2)2NMe2 phenethyl 8.2 1.0
6 H -(CH2)3NH2 phenethyl 6.5 0.5
7 H -(CH2)3NMe2 phenethyl 7.8 1.0
8 H -(CH2)3N(Me)iPr 3-chlorophenethyl 8.3 0.8
9 H -(CH2)3N(Me)Et 3-chlorophenethyl 8.0 0.8
10 H -(CH2)3N(Me)cyPr 3-chlorophenethyl 8.1 0.8
11 H -(CH2)2-piperidin-1-yl 3-chlorophenethyl 7.9 0.7
12 H -(CH2)2NEt2 2-(naphthalen-1-yl)ethyl 8.2 0.8
13 H -(CH2)2NEt2 2-(naphthalen-2-yl)ethyl 8.0 0.5
14 H -(CH2)2NEt2 3-fluorophenethyl 8.1 0.8
15 H -(CH2)2NEt2 3-methoxyphenethyl 8.1 0.6
16 H -(CH2)2NEt2 3-chlorophenethyl 8.2 0.7
a

β2AR agonism was performed in H292 cells (bronchial epithelial cell line) expressing the human β2 adrenergic receptor. Functional activity was determined by measuring accumulation of intracellular cAMP using AlphaScreen. The compounds were incubated for 1 h at 22 °C.

b

IA (Intrinsic activity) measured relative to formoterol (pEC50 8.6, IA = 1).