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. 2020 Sep 25;21(19):7088. doi: 10.3390/ijms21197088

Table 1.

Sigma1R ligand with antidepressant properties.

Compound Sigma1R Activity Sigma1R Affinity, Ki
Inline graphic
Fluvoxamine
Agonist
[23,26,31,93,94,95,96]
36.0 nM [21]
17.0 nM [23]
Inline graphic
Fluoxetine
Putative agonist
[23,91,92,93,97]
240.0 nM 1 [21]
191.2 nM [23]
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Sertraline
Putative antagonist
Putative inverse agonist
[91,92,93,94,98]
57.0 nM [21]
31.6 nM [23]
Inline graphic
Escitalopram
Agonist
[23,93]
288.3 nM [23]
Inline graphic
Citalopram
Agonist
[99]
292.0 nM [21]
403.8 nM [23]
Inline graphic
Imipramine
Agonist
[95,100,101,102]
343.0 nM [21]
332.1 nM [101]
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DHEA
Agonist
[103,104,105]
2.96 μM [106]
706.0 nM [107]
Inline graphic
Igmesine (JO-1784)
Agonist
[92,108]
75.0 nM [109]
Inline graphic
Cutamesine (SA4503)
Agonist
[93,110]
17.4 nM 2 [111]
Inline graphic
Ketamine
Putative agonist
[101,112]
139.6 μM 3 [101]

1 Ki for (±)-fluoxetine; 2 IC50 3 Ki for (±)-ketamine.