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. Author manuscript; available in PMC: 2019 Jun 1.
Published in final edited form as: Pharmacol Ther. 2018 Jan 31;186:152–167. doi: 10.1016/j.pharmthera.2018.01.009

Table 1.

Ligand Affinities for σ1R, σ2R, and DAT (Ki, nM)

Stimulants and Psychiatric Drugs
Ligand Activity σ1R σ2R DAT Reference
Cocaine Agonist n.d. n.d. 164 Izenwasser et al., 1999
5,190 19,300 77 Garcés-Ramírez et al., 2012
1,347 48,170 n.d. Lever et al., 2016
Fluoxetine Agonist 240 16,100 n.d. Narita et al., 1996
Haloperidol Antagonist 7.0 n.d. n.d. Su, 1982
1.9 79.8 n.d. Bowen et al., 1993
n.d. n.d. 5,232 Izenwasser et al., 1993
3.3 270.0 n.d. Takahashi et al., 1999
2.2 16.0 9,578 Moison et al., 2003
0.9 7.9 n.d. Lever et al., 2006
1.2 18.1 n.d. Lever et al., 2014
1.4 72.8 n.d. Lever et al., 2016
Methamphetamine ??? †2,160 †46,670 n.d. Nguyen et al., 2005
4,390 15,900 n.d. Hiranita et al., 2013
MDMA ??? 3,057 8,889 10,320 Brammer et al., 2006
Sertraline Agonist 57 5,297 n.d. Narita et al., 1996
Selective σ Ligands
Ligand Activity σ1R σ2R DAT Reference
(+)-3-PPP Agonist 49.3 120.0 n.d. Bowen et al., 1993
n.d. n.d. 1,784 Izenwasser et al., 1993
AC927 Antagonist 30.0 138.0 2,939 Matsumoto et al., 2008
AZ66 Antagonist 2.4 0.5 872 Seminerio et al., 2012
4.7 1.4 1,950 Katz et al., 2016
BD1008 Antagonist 2.0 8.0 n.d. McCrackena et al., 1999
2.1 16.6 2,510 Garcés-Ramírez et al., 2012
BD1047 Antagonist 0.9 47.0 n.d. Matsumoto et al., 1995
3.0 48.0 3,220 Garcés-Ramírez et al., 2012
BD1063 Antagonist 9.2 449.0 n/a Matsumoto et al., 1995
6.0 440.0 16,820 Brammer et al., 2006
9.0 625.0 8,020 Garcés-Ramírez et al., 2012
8.8 626.0 8,020 Katz et al., 2016
9.7 762.0 n.d. Lever et al., 2016
BMY-14802 Antagonist 265.0 391.0 n.d. Weigl et al., 2002
CM156 Antagonist 1.3 0.6 1,175 Xu et al., 2010
DTG Agonist 74.3 61.2 n.d. Bowen et al., 1993
69.0 21.0 >10,000 Moison et al., 2003
35.5 39.9 n.d. Lever et al., 2006
57.0 22.0 93,500 Garcés-Ramírez et al., 2012
111.8 39.1 n.d. Lever et al., 2016
MR200 Agonist 1.5 21.9 >10,000 Moison et al., 2003
MS-377 Antagonist 73.0 6,900.0 n.d. Takahashi et al., 1999
NE100 Antagonist *1.5 *633.0 n.d. Chaki et al., 1994
2.5 121.0 3,590 Hiranita et al., 2011
(+)-Pentazocine Agonist 6.7 1,361 n.d. Bowen et al., 1993
1.6 728.4 n.d. Lever et al, 2006
4.6 224.0 n.d. Hiranita et al., 2013
5.1 2,060.0 n.d. Lever et al., 2016
PRE-084 Agonist *44.0 n.d. n.d. Su et al., 1991
n.d. n.d. 5,344 Izenwasser et al., 1993
46.5 n.d. n.d. Cao et al., 2003
48.5 12,700.0 n.d. Hiranita et al., 2013
53.0 32,100.0 19,600 Garcés-Ramírez et al., 2012
SA4503 Agonist *17.4 *1,784.0 n/a Matsuno et al., 1996
4.6 63.1 n.d. Lever et al., 2006
(+)-SKF-10,047 Agonist 28.7 33,654.0 n.d. Bowen et al., 1993
Other Drugs
Ligand Activity σ1R σ2R DAT Reference
DHEA-sulfate Agonist 15,129 n.d. n.d. Maurice et al., 1996
DMT ??? †14,750 †21,710 n.d. Fontanilla et al., 2009
PCP ??? *2,541 n.d. n.d. Su, 1982
Progesterone Antagonist 175 n.d. n.d. Maurice et al., 1996
2.7 n.d. n.d. Su et al., 1988
Rimacozole Antagonist 908.0 302.0 224 Husbands et al., 1999
96.6 883.0 238 Hiranita et al., 2011

n.d.: not determined,

†

KD,

*

IC50