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

Table 2. Binding Affinities of Guanidino-piperidines 7b, 17ag 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  
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.

b

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.