Table 3. Binding Affinities of Guanidino-piperidines 26, 30a–d, 34, 42−43, 46, and 49a–g 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 | |
21 | 319 ± 19 | 405 ± 56 | |
26 | 904 ± 237 | 1893 ± 490 | |
30a | 94 ± 24 | 309 ± 55 | 3.3-fold (NPFF1) |
30b | 114 ± 17 | 987 ± 65 | 8.7-fold (NPFF1) |
30c | 201 ± 35 | 884 ± 177 | 4.4-fold (NPFF1) |
30d | 191 ± 31 | 409 ± 39 | 2.1-fold (NPFF1) |
34 | 511 ± 79 | 3505 ± 847 | 6.9-fold (NPFF1) |
42 | 417 ± 74 | 84 ± 12 | 5-fold (NPFF2) |
43 | 151 ± 15 | 465 ± 108 | 3-fold (NPFF1) |
46 | 81 ± 17 | 1426 ± 49 | 17.6-fold (NPFF1) |
49a | 15085 ± 355 | 2757 ± 81 | |
49b | 1638 ± 499 | 298 ± 14 | 5.5-fold (NPFF2) |
49c | 1057 ± 150 | 330 ± 28 | 3.2-fold (NPFF2) |
49d | 538 ± 40 | 129 ± 26 | 4.2-fold (NPFF2) |
49e | 141 ± 34 | 504 ± 95 | 3.6-fold (NPFF1) |
49f | 112 ± 11 | 454 ± 4 | 4-fold (NPFF1) |
49g | 340 ± 91 | 1513 ± 33 | 4.5-fold (NPFF1) |
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 to four experiments performed in duplicate.