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. 2023 Aug 3;66(16):11447–11463. doi: 10.1021/acs.jmedchem.3c00959

Table 1. S1R and S2R Binding Assays.

graphic file with name jm3c00959_0010.jpg

      Ki (nM) ± SDa
ID n m S1R S2R KiS2R/KiS1R
7b 0 0 10 ± 1.4 40 ± 4.4 4.0
8a 0 1 6.5 ± 0.9 95 ± 9.5 14.6
8b 0 2 8.6 ± 1.4 85 ± 13 9.9
11b 1 0 1.8 ± 0.4 14 ± 1.6 7.8
13a 1 1 2.5 ± 0.4 20 ± 3.1 8.0
13b 1 2 11 ± 2.0 12 ± 2.3 1.1
14a 2 1 2.1 ± 0.4 13 ± 2.2 6.2
14b 2 2 11 ± 1.4 18 ± 3.4 1.6
16c 3 2 36 ± 5.7 7.7 ± 0.7 0.2
(+)-PTZ     4.3 ± 0.5 1465 ± 224  
DTG     124 ± 19 18 ± 1  
Haloperidol     2.6 ± 0.4 77 ± 18  
BD1063     14 ± 2.7 204 ± 31  
a

Each value is the mean ± SD of at least two experiments performed in duplicate.