4-aroylpiperidines and 4-(α-hydroxyphenyl)piperidines as selective sigma-1 receptor ligands: synthesis, preliminary pharmacological evaluation and computational studies

Table 1 Binding affinity of methanone analogues

Compound	R	σ₁ (K _i nM)	σ₂ (K _i nM)	Selectivity ratio (K _i σ₂/σ₁)
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
Spipethiane^a		0.50	416	208
(+)-pentazozcine^b		3.58	1932	540

ISSN: 2661-801X