. Author manuscript; available in PMC: 2017 Mar 1.

Published in final edited form as: Synapse. 2015 Dec 24;70(3):98–111. doi: 10.1002/syn.21877

TABLE II.

Sigma receptor binding parameters and subtype selectivity for a panel of ligands in CD-1^® mouse whole brain membranes^a

Compound	IC₅₀ (nM)	^b Sigma₁K_i (nM)	n_H	IC₅₀ (nM)	^c Sigma₂K_i (nM)	n_H	Selectivity K_i Ratio σ₂/σ₁
Ifenprodil	35.03 ± 0.95	22.68 ± 0.61	1.08 ± 0.06	2.69 ± 0.36	2.43 ± 0.32	0.70 ± 0.07	0.1
(+)-Pentazocine	7.88 ± 0.53	5.10 ± 0.34	1.09 ± 0.03	2280 ± 167	2060 ± 151	0.86 ± 0.04	404
DTG	172.7 ± 19.88	111.8 ± 12.86	0.91 ± 0.14	43.3 ± 3.2	39.1 ± 2.8	0.88 ± 0.05	0.35
BD1063	9.68 ± 1.00	5.98 ± 0.62	1.17 ± 0.08	843 ± 104	762 ± 94	0.96 ± 0.13	127
(−)-Cocaine	2074 ± 341	1347 ± 221	1.00 ± 0.11	53420 ± 4154	48170 ± 3748	1.03 ± 0.05	36
(−)-Cocaine^d	1359 ± 53	1075 ± 42	0.91 ± 0.11
E-IA-DM-PE-PIPZE	10.39 ± 1.39	6.73 ± 0.90	0.98 ± 0.07	1604 ± 243	1447 ± 220	0.98 ± 0.08	215
Dextromethorphan	97.5 ± 6.9	63.1 ± 4.5	0.88 ± 0.07	29970 ± 2823	26810 ± 2525	1.02 ± 0.07	425
Haloperidol	2.12 ± 0.22	1.35 ± 0.12	0.94 ± 0.03	80.7 ± 12.9	72.8 ± 11.6	1.12 ± 0.06	54
(+)-NANM	20.55 ± 1.14	13.30 ± 0.74	1.06 ± 0.11	8991 ± 850	8095 ± 765	0.98 ± 0.12	608
(−)-NANM	3985 ± 600	2551 ± 383	1.09 ± 0.08	7465 ± 469	6720 ± 422	0.93 ± 0.08	2.6

Values are means ± SEM, n = 3 – 6.

3.0 nM [³H](+)pentazocine, 37 °C, 180 min, 1.0 μM haloperidol defined non-specific binding.

3.0 nM [³H]DTG/500 nM (+)pentazocine, 25 °C, 60 min, 10.0 μM haloperidol defined non-specific binding.

1.0 nM [¹²⁵I]E-IA-DM-PE-PIPZE, 37 °C, 60 min, 1.0 μM haloperidol defined non-specific binding.