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. 2022 Aug 8;23(15):8797. doi: 10.3390/ijms23158797

Table 1.

Receptor binding affinities (mean ± SEM) at recombinant rat iGluRs.

cmpd R Ki (µM)
GluK1 GluK2 GluK3 GluK5 GluA2
DNQX 1 0.65 ± 0.03 2.1 ± 0.3 0.36 ± 0.03 7.1 ± 0.9 0.25 ± 0.01
NBQX 2.6 ± 0.1 5.4 ± 1.2 3.4 ± 0.6 152 ± 23 0.077 ± 0.010
1 2 Ph >100 ≈100 2.9 ± 0.3 >100 24 ± 6
5 3-Me-Ph ≈100 ≈100 1.4 ± 0.4 >100 >100
6 4-Me-Ph ≥100 nd 6.1 ± 0.8 nd nd
7 4-Et-Ph >100 >100 20 ± 1 >100 >100
8 4-nPr-Ph >100 >100 50 ± 12 >100 >100
9 4-iPr-Ph >100 >100 38 ± 10 >100 >100
10 4-Cl-Ph >100 >100 3.5 ± 0.7 >100 >100
11 4-CF3-Ph ≈100 >100 >100 >100 >100
12 4-MeO-Ph >100 >100 8.3 ± 0.4 >100 >100
13 4-PhO-Ph ≥100 nd 7.9 ± 0.7 nd nd
14 3-COOH-Ph >100 >100 28 ± 2 >100 >100
15 4-COOH-Ph >100 >100 31 ± 4 >100 >100
16 4-NH2SO2-Ph >100 >100 ≈100 >100 >100
17 4-FSO2-Ph 1.1 ± 0.4 >100 8.1 ± 0.4 >100 ≈100
18 2-OH-Ph >100 nd 14 ± 2 nd nd
19 3-OH-Ph >100 >100 3.2 ± 0.6 >100 ≈100
20 4-OHCH2-Ph ≈100 >100 5.8 ± 1.5 >100 >100
21 2-NH2-Ph 14 ± 2 nd 1.0 ± 0.1 nd nd
22 3-NH2-Ph >100 nd ≈100 nd nd
23 4-NH2-Ph >100 >100 1.4 ± 0.2 >100 >100
24 4-N(CH3)2-Ph 39 ± 4 nd 24 ± 4 nd nd
25 pyridin-4-yl >100 >100 25 ± 6 >100 >100
26 6-hydroxypyridin-3-yl >100 >100 11 ± 1 >100 >100
27 pyrimidin-5-yl 11 ± 2 12 ± 2 0.28 ± 0.02 >100 >100
28 graphic file with name ijms-23-08797-i001.jpg ≈100 >100 0.25 ± 0.01 >100 >100
29 graphic file with name ijms-23-08797-i002.jpg 0.15 ± 0.05 0.091 ± 0.015 0.13 ± 0.03 3.8 ± 0.1 0.23 ± 0.02

1 Data from the reference [34]; 2 Data from the reference [33]; nd—not determined.