Table 2. Activity of Bi-aryl Sulfonamidesa.
I30μM/Icontrol (mean ± SEM, %) IC50 (μM)b |
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---|---|---|---|---|---|---|---|
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 |
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.
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.