Table 1.

Sigma receptor affinity of norbenzomorphan analogs.

Cmpd	R1	R2	Sig1R Ki(nM)a pKi ± SEMb	Sig2R Ki(nM) pKi ± SEM	Ki(Sig1R)/Ki(Sig2R)
12	Cl		* c	*	-
16			*	*	-
20			3,777 5.42 ± 0.09	1,034 5.99 ± 0.07	4
39			2,975 5.53 ± 0.09	92 7 ± 0.1	32
40			4,544 5.34 ± 0.09	1,258 5.9 ± 0.1	4
19			2,429 5.61 ± 0.06	318 6.5 ± 0.1	8
38			3,519 5.5 ± 0.1	746 6.1 ± 0.1	5
27			3,039 5.5 ± 0.1	723 6.14 ± 0.09	4
41		CH3	156 6.81 ± 0.09	43 7.36 ± 0.08	4
42			1,058 6.0 ± 0.1	166 6.8 ± 0.1	6
43		CH3	391 6.41 ± 0.08	133 6.88 ± 0.07	3
44			4,612 5.34 ± 0.08	828 6.08 ± 0.08	6
SAS-0132 (32)			497 6.31 ± 0.06	71 7.1 ± 0.1	7
33		H	*	*	-
34			442 6.36 ± 0.06	27 7.58 ± 0.08	16
35			*	764 6.12 ± 0.07	-
36			294 6.53 ± 0.08	357 6.45 ± 0.06	1
37			2105 5.68 ± 0.07	442 6.37 ± 0.07	5
28			589 6.23 ± 0.06	34 7.47 ± 0.08	17
29			172 6.76 ± 0.05	16 7.79 ± 0.05	11
30			62 7.21 ± 0.05	23 7.64 ± 0.07	3
SAS-1121 (31)			9294d 5.1 ± 0.1	16.2e 7.8 ± 0.16	574

^aK_i values obtained from non-linear regression of radioligand competition binding isotherms;

^bSEM calculated for pK_i;

^cLess than 50% inhibition of radioligand binding with 10 μM test ligand;

^daverage of two IC₅₀ determinations;

^eaverage of three IC₅₀ determinations.