Table 10.
Agonist Activity of 2-(N-piperazinyl)acetamides 54-61 [79]
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# | R1 | R2 | R3 | R4 | EC50 (μM)a | ||
FPR1 | FPR2 | PMN | |||||
54 | H | H | F | H | N.A. | 19.3 | 10.5 |
55 | H | Cl | H | H | N.A. | 15.1 | 16.4 |
56 | H | H | H | H | N.A. | 8.7 | 2.3 |
57 | H | H | Cl | H | N.A. | 2.1 | 2.0 |
58 | H | Cl | CH3 | H | N.A. | 4.3 | 1.0 |
59 | CH3 | Cl | H | H | N.A. | 4.1 | 1.8 |
60 | CH3 | H | H | Cl | N.A. | 9.4 | 0.4 |
61 | H | OCH3 | H | H | N.A. | 11.0 | 7.9 |
EC50 values were determined by measurement of Ca2+ flux in FPR1- and FPR2-transfected RBL cells or in human polymorphonuclear neutrophils (PMN). N.A., no activity observed.