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. 2014 Sep 30;57(21):8903–8927. doi: 10.1021/jm500989n

Table 3. Binding Affinities of Guanidino-piperidines 26, 30ad, 34, 4243, 46, and 49ag 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)
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 to four experiments performed in duplicate.