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. Author manuscript; available in PMC: 2016 Jul 15.
Published in final edited form as: Bioorg Med Chem. 2014 Dec 13;23(14):3913–3924. doi: 10.1016/j.bmc.2014.12.007

Table 1.

Effect of the compounds on Ca2+ mobilization in FPR1/FPR2 transfected cells, human and mouse neutrophils

graphic file with name nihms649342t1.jpg

Compound FPR1 FPR2 Human PMN
(w/o
probenecid)
Human PMN
(with
probenecid)
Mouse PMN

EC50, µM (Efficacy, %)

(S)-9a 0.43 ± 0.13
(130)
0.096 ± 0.027
(120)
0.064 ± 0.026
(100)
0.060 ± 0.021
(105)
0.24 ± 0.07
(110)

(R)-9a N.A. 0.23 ± 0.083
(100)
0.92 ± 0.28
(40)
0.88 ± 0.25
(95)
4.9 ± 1.4
(30)

(S)-9b N.A. 1.6 ± 0.36
(115)
12.6 ± 3.7
(55)
0.66 ± 0.18
(130)
1.7 ± 0.44
(50)

(R)-9b N.A. N.A. N.A. N.A. 2.3 ± 0.73
(65)

(S)-9c N.A. N.A. N.A. N.A. 2.5 ± 0.61
(60)

(R)-9c N.A. 0.26 ± 0.064
(65)
N.A. 0.97 ± 0.34
(40)
3.8 ± 1.3
(35)

(S)-9d N.A. 0.73 ± 0.23
(75)
1.8 ± 0.42
(30)
0.27 ± 0.082
(105)
3.9 ± 1.5
(75)

(R)-9d N.A. N.A. N.A. N.A. 2.1 ± 0.58
(80)

(S)-9e 0.95 ± 0.26
(115)
0.43 ± 0.11
(135)
1.8 ± 0.37
(85)
0.45 ± 0.13
(120)
2.8 ± 0.64
(80)

(R)-9e N.A. 0.31 ± 0.092
(90)
0.62 ± 0.24
(40)
0.49 ± 0.16
(115)
1.0 ± 0.27
(55)

(S)-9f N.A. 0.86 ± 0.21
(40)
N.A. 1.1 ± 0.36
(55)
2.3 ± 0.35
(25)

(R)-9f N.A. N.A. N.A. N.A. 2.5 ± 0.42
(25)