Table 1.

Nomenclature, chemical structures and comparison of affinity values generated in whole tissue and from a cloned human Sigma-1 receptor expressed in MCF-7 cells. Affinity values (K_i or K_D, nM) are expressed a geometric means ± standard deviations. Average K_i values from available past studies using whole tissues are listed for comparison.A superscripted letter next to individual values indicates the reference, which is listed below.

Compound Names and Structures	Ki values for the cloned hSigma-1 receptor	Ki values measured in whole tissues	Average Ki values from whole tissues
Sigma-1 Receptor Reference Compounds
	3.11 ± 2.40	9.15 i	9
	250 ± 79.1	19.4 a	205 ± 339
		48 d
		713 b
		41 l
	7132 ± 2551	84.9 a	2247 ± 2104
		1800 d
		5133 b
		1970 l
	3.70 ± 0.872	17 b	8 ± 8
		4.59 a
		1 l
	173 ± 58.2	306 b	186 ± 170
		66 m
	54.7 ± 23.9	9 n	9
	0.903 ± 0.397	1.14 h	1.14
	5.29 ± 0.978	2.57 c	8 ± 7
		13.1 j
Butyrophenone Antipsychotics and Metabolites
	1.67 ± 0.801	3.12 a	4 ± 3
		0.2 l
		1.47 g
		4 d
		3 m
		10.2 b
		2.7 p
	128 ± 20.6	362 m	344 ± 25
		326 p
	1.54 ± 0.817	22 m	14 ± 12
		5.1 p
	>10,000	>10,000 m	>10,000
	3.32 ± 0.0954	12 m	12
	1.18 ± 0.355	-	-
	1.28 ± 0.628	-	-
	2241 ± 864	-	-
	241 ± 64.1	-	-
	1054 ± 579	1090 d	1090
	147 ± 39.5	-	-
Antipsychotics/Antidepressants
	159.0 ± 57.4	144 d	736 ± 733
		508 o
		1,555 m
	53.8 ± 25.2	-	-
	13.9 ± 4.68	17 d	63 ± 46
		62 o
		109 m
	>10,000	11400 d	>10,000
		>10,000 m
	7.09 ± 3.18	36 e	36
D4 Dopamine Receptor Selective Ligands
	63.0 ± 22.7	-	-
	4.80 ± 0.919	-	-
	2.48 ± 0.580	-	-
	5161 ± 2670	-	-
	2612 ± 269	-	-
Drugs of Abuse
	5248 ± 1044	2160 f	2160
	>100,000	-	-
	>100,000	-	-
Endogenous Neurosteroids
	468 ± 139	268 g	235 ± 143
		24.6 a
		338 l
		338 q
	>10,000	-	-

^aMcCann et al. (1994).

^bKarasawa et al (2000).

^cJohn et al. (1993).

^dTam et al. (1984).

^eNarita et al. (1996).

^fNguyen et al. (2005).

^gSu (1988).

^hHashimoto and London (1993).

ⁱMatsumoto et al. (1995).

^jJohn et al. (1999).

^lHanner et al. (1996).

^mMatsumoto et al. (2000).

ⁿBrown et al. (2004).

^oLargent et al. (1984).

^pBowen et al. (1990).

^qRamamoorthy et al. (1995).