Table 1.
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 | ≈100 | >100 | 0.25 ± 0.01 | >100 | >100 | |
29 | 0.15 ± 0.05 | 0.091 ± 0.015 | 0.13 ± 0.03 | 3.8 ± 0.1 | 0.23 ± 0.02 |