Table 1. In Vitro Pharmacology for Compounds 7 and 8.
| human FLIPR pIC50a | rat FLIPR pIC50b | mouse FLIPR pIC50c | human pKi | rat pKi | rat/human SERTd pKi (nM) | human PBMC pIC50e | human WB pIC50f | |
|---|---|---|---|---|---|---|---|---|
| 7 | 8.3 ± 0.08 | 7.2 ± 0.08 | 7.5 ± 0.1 | 7.9 ± 0.08 | 8.7 ± 0.08 | 5.5/n.d. | 7.6 ± 0.07 | 6.7 ± 0.07 |
| 8 | 7.7 ± 0.07 | 7.8 ± 0.1 | 7.1 ± 0.2 | 7.9 ± 0.08 | 9.1 ± 0.07 | 7.7 (n = 2)/7.8 | 7.4 ± 0.07 | 6.7 ± 0.09 |
a
Human FLIPR pIC50 measured in a Ca2+ flux assay.
b
Rat FLIPR pIC50 measured in a Ca2+ flux assay.
c
Mouse FLIPR pIC50 measured in a Ca2+ flux assay.
d
Rat and human SERT Ki.
e
Human peripheral blood monocyte pIC50 for IL-1b inhibition.
f
Human whole blood pIC50, all data are the result of at least three assays run in triplicate ± SEM.