Table 4. Binding Affinities of Guanidino-piperidines 53a–d at NPFF1-R and NPFF2-Ra.
| cmpd | hNPFF1-R (Ki, nM) | hNPFF2-R (Ki, nM) | ratio |
|---|---|---|---|
| NPVF | 3.66 ± 0.95 | ||
| 1DMe | 3.85 ± 0.42 | 0.47 ± 0.08 | |
| 42 | 417 ± 74 | 84 ± 12 | 5-fold (NPFF2) |
| 53a | 112 ± 19 | 30 ± 5 | 3.7-fold (NPFF2) |
| 53b | 432 ± 14 | 82 ± 8 | 5.3-fold (NPFF2) |
| 53c | 316 ± 11 | 205 ± 8 | 1.5-fold (NPFF2) |
| 53d | 296 ± 14 | 910 ± 107 | 3-fold (NPFF1) |
a
Ki values were determined by using [3H]NPVF and [3H]EYF for hNPFF1-R and hNPFF2-R, respectively, and are the mean ± SEM from two-four experiments performed in duplicate.