Table 3. Comparison of Sulfonamide to Amide Linkera.
Idrug/Icontrol (mean ± SEM, %)b, IC50 (μM)c |
|||||
---|---|---|---|---|---|
Cmpd # | cLogPd | Drug μM | GluN2A | GluN2C | GluN2D |
9 | 3.55 | 6 | 5.1 ± 1.3 | ND | ND |
0.17 | |||||
26 | 4.22 | 30 | 102 ± 2.2 | ND | ND |
ND | |||||
23 | 4.34 | 30 | 85 ± 1.2 | 9.0 ± 2.8 | 8.9 ± 2.3 |
ND | 2.4 | 1.7 | |||
27 | 4.59 | 30 | 82 ± 8.6 | 56 ± 1.9 | 49 ± 1.6 |
ND | 37 | 29 |
Data are from 8 to 9 oocytes from 2 frogs for each compound tested.
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.
IC50 values were determined by fitting the Hill equation to the average composite concentration–response curve and are reported to two significant figures. ND indicates not determined.
cLogP calculated using Chemicalize from ChemAxon.