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. 2019 Jan 4;10(3):248–254. doi: 10.1021/acsmedchemlett.8b00395

Table 2. Activity of Bi-aryl Sulfonamidesa.

graphic file with name ml-2018-003954_0006.jpg

            I30μM/Icontrol (mean ± SEM, %) IC50 (μM)b
Cmpd #   n R1 R2 Y GluN2C GluN2D
16 para 1 H H CH 42 ± 2.5 20 ± 2.5
22 10
17 para 1 H H N 58 ± 4.6 45 ± 3.3
35 24
18 meta 1 H H CH 60 ± 2.0 46 ± 2.6
45 29
19 meta 1 H H N 52 ± 1.4 42 ± 1.3
34 23
20 para 2 H H CH 77 ± 2.9 67 ± 4.4
ND ND
21 para 2 H H N 37 ± 2.8 26 ± 4.1
12 5.1
22 para 2 Cl F CH 79 ± 1.4 74 ± 2.0
ND ND
23 meta 2 H H CH 9.0 ± 2.8 9.0 ± 2.3
2.4 1.7
24 meta 2 H H N 8.5 ± 1.3 8.6 ± 1.4
3.2 2.7
25 meta 2 Cl F CH 41 ± 1.6 28 ± 2.6
2.4 1.3
a

The response to drug coapplied with a maximally effective concentration of glutamate (100 μM) and glycine (30 μM) is given as a percent of the control response to glutamate and glycine alone.

b

Fitted IC50 values are reported to two significant figures; inhibition in saturating test compound was set to 0 for all except 16, which was 41% for GluN2C and 27% for GluN2D. ND indicates not determined. Data are from 8 to 16 oocytes from 2 to 3 frogs for each compound and receptor tested.