In vitro activity of NPFF receptor agonists at human FF1 and FF2 receptors as measured by R-SAT, cAMP, and binding assays
Efficacy values are expressed relative to the internal reference standards, NPAF and NPFF, for FF1 and FF2 receptors, respectively (R-SAT) and NPFF (cAMP).
| Compound | R-SAT | cAMP | Binding Ki | |||||||
|---|---|---|---|---|---|---|---|---|---|---|
| hFF2 | hFF1 | hFF2 | hFF1 | hFF2 | hFF1 | |||||
| %Eff | pEC50 | %Eff | pEC50 | %Eff | pEC50 | %Eff | pEC50 | |||
| nM | ||||||||||
| NPAF | 105 ± 16 | 8.7 ± 0.6 | 100 | 6.6 ± 0.4 | 8.5 ± 0.6 | 100 | 7.2 ± 0.3 | 3.2 ± 4.0 | 9.8 ± 0 | |
| NPFF | 100 | 6.5 ± 0.3 | N.T. | 100 | 8.2 ± 0.4 | 7.3 ± 0.4 | 0.98 ± 1.1 | 0.9 ± 0 | ||
| AC-262616 | 73 ± 13 | 7.0 ± 0.4 | 52 ± 3a | <7.4 | 114 ± 8 | 5.5 ± 0 | 93 ± 9 | 5.9 ± 0.1 | 230 ± 11 | 172 ± 160 |
| AC-263093 | 90 ± 15 | 5.9 ± 0 | 12 ± 0a | N.D. | 78 ± 24 | 5.2 ± 0.3 | 23 ± 9a | N.D. | 1296 ± 942 | 3320 ± 2890 |
%Eff, percent efficacy; N.D., could not be determined; N.T., not tested.
↵a %Eff values reported are those obtained at the highest testable concentration of compound (6 μM for RSAT and 30 μM for cAMP assays). Because of the toxicity of the compound, higher concentrations could not be tested for these compounds. Because proper dose-response could not be constructed, potency of these compounds has been estimated.