Affinity values (Ki, nM) of selected chromenones at the human σ (hσ1) and rat σ2 (rσ2) receptors.
Compd | R | n | hσ1 | rσ2 | Selectivity hσ1//rσ2 |
---|---|---|---|---|---|
1 | 1 | 2870 | 12 500 | 4.4 | |
2 | 2 | 499 | 23 900 | 48 | |
3 | 3 | 227 | 3110 | 14 | |
4 | 4 | 87.0 | 1450 | 17 | |
5 | 1 | 825 ± 146 | 9070 | 11 | |
6 | 2 | 65.5 ± 4.5 | 2890 | 44 | |
7 | 3 | 309 ± 45 | 1970 ± 1400 | 6.4 | |
8 | 4 | 213 | 490 | 2.3 | |
9 | 1 | >10 000 | >10 000 | n.d. | |
10 | 2 | 245 | 22 500 | 92 | |
11 | 3 | 23.9 ± 9.7 | 14 600 | 610 | |
12 | 4 | 19.6 ± 3.2 | 2630 ± 1200 | 130 | |
13 | 1 | 604 | 14 200 | 24 | |
14 | 2 | 809 | 17 100 | 21 | |
15 | 4 | 82.5 | 4100 | 50 | |
16 | 1 | 12 100 | 30 000 | 2.5 | |
17 | 2 | 1220 | 8360 | 6.9 | |
18 | 4 | 218 | 2500 | 11 | |
19 | 1 | 113 ± 28 | 1620 | 14 | |
20 | 2 | 27.2 ± 6.8 | 750 ± 250 | 28 | |
21 | 3 | 104 | 1090 | 10 | |
22 | 4 | 134 | 583 | 4.4 | |
Haloperidol | 3.53 ± 0.47 | 20.5 ± 1.0 | 5.8 | ||
SA4503 | 3.77 ± 0.11 | n.d.a | n.d. | ||
S1RA b | 17.0 | 9300 | 550 |
Not determined.
Data from ref. 21.