Table 2. Sigma Receptor Affinities (Ki ± SD [nM]) of Selected Analogs.
D3 | σ1 | σ2 | D3/ σ1 Ratio | D3/ σ2 ratio | |
---|---|---|---|---|---|
1 | 0.8 ± 0.1 | 1,260 ± 290 | 1,570 ± 310 | 1,573 | 1,970 |
2 | 2.4 ± 0.4 | 3,540 ± 2500 | 2,210 ± 260 | 1,476 | 919 |
18a | 1.1 ± 0.1 | 4,780 ± 730 | 660 ± 36 | 4344 | 601 |
18c | 4.2 ± 0.2 | 4,870 ± 470 | 1,120 ± 30 | 1,159 | 266 |
20a | 0.65 ± 0.2 | 1,960 ± 50 | 650 ± 38 | 3,017 | 1,002 |
20c | 0.52 ± 0.03 | 4,360 ± 570 | 794 ± 14 | 8,377 | 1,527 |
20e | 0.17 ± 0.01 | 20,900 ± 5250 | 5,960 ± 360 | 122,706 | 35,047 |
21b | 1.1 ± 0.2 | 7,200 ± 880 | 2,020 ± 260 | 6,541 | 1,839 |
21e | 1.1 ± 0.2 | 7,780 ± 540 | 1,320 ± 33 | 7,076 | 1,200 |
Haloperidol | – | 1.5 ± 0.3 | 24.2 ± 3.0 | – | – |