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Table 1 Binding affinity of methanone analogues

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 σ21)
7a 4″-F 2.96 ± 0.5 221.64 ± 8.0 75
7b 3″,4″-Cl2 >434 >854 2
7c 4″-Cl 5.98 ± 0.41 554.03 ± 34.22 93
7d 2″-NO2 >434 >854 2
7e 4″-Br 1.40 ± 0.5 >854 610
7f 4″-Me 11.58 ± 0.26 151.47 ± 7.79 13
Spipethianea 0.50 416 208
(+)-pentazozcineb 3.58 1932 540
  1. aData available from Ref. [24]
  2. bData available from Ref. [24]