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. 2021 May 20;12(6):1000–1004. doi: 10.1039/d1md00105a

Affinity values (Ki, nM) of selected chromenones at the human σ (hσ1) and rat σ2 (rσ2) receptors.

graphic file with name d1md00105a-u1.jpg
Compd R n 1 2 Selectivity hσ1//rσ2
1 graphic file with name d1md00105a-u2.jpg 1 2870 12 500 4.4
2 2 499 23 900 48
3 3 227 3110 14
4 4 87.0 1450 17
5 graphic file with name d1md00105a-u3.jpg 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 graphic file with name d1md00105a-u4.jpg 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 graphic file with name d1md00105a-u5.jpg 1 604 14 200 24
14 2 809 17 100 21
15 4 82.5 4100 50
16 graphic file with name d1md00105a-u6.jpg 1 12 100 30 000 2.5
17 2 1220 8360 6.9
18 4 218 2500 11
19 graphic file with name d1md00105a-u7.jpg 1 113 ± 28 1620 14
20 2 27.2 ± 6.8 750 ± 250 28
21 graphic file with name d1md00105a-u8.jpg 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
a

Not determined.

b

Data from ref. 21.