From: 4-aroylpiperidines and 4-(α-hydroxyphenyl)piperidines as selective sigma-1 receptor ligands: synthesis, preliminary pharmacological evaluation and computational studies
Compound
R
σ1 (K i nM)
σ2 (K i nM)
Selectivity ratio (K i σ2/σ1)
8a
4″-F
1.41 ± 0.22
>854
606
8b
3″,4″-Cl2
>434
2
8c
4″-Cl
2.49 ± 0.24
343
8d
2″-NO2
526.53 ± 69
8e
4″-Br
5.22 ± 0.3
164
8f
4″-Me
1.45 ± 0.4
589