Table 2. Binding Affinities of Guanidino-piperidines 7b, 17a–g and 21 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 | |
7bb | 487 ± 117 | 1052 ± 32 | 2.2-fold (NPFF1) |
17a | 441 ± 14 | 2907 ± 216 | 6-fold (NPFF1) |
17b | 3429 ± 377 | 3220 ± 53 | |
17cb | 2692 ± 121 | 2682 ± 570 | |
17db | 2454 ± 338 | 2223 ± 388 | |
17eb | 1623 ± 630 | 993 ± 87 | |
17fb | 1966 ± 324 | 1620 ± 179 | |
17gb | 2348 ± 413 | 2398 ± 288 | |
21 | 319 ± 19 | 405 ± 56 |
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.
Ki values were determined by using [125I]YVP and [125I]EYF for hNPFF1-R and hNPFF2-R, respectively, and are the mean ± SEM from two to four experiments performed in duplicate.