Table 3.
Concentration-dependent inhibition of radioligand binding to SURs by DOGS-NTA in the presence of MgATP (0.3 mM)
| SUR | Radioligand | IC50 (μM) | A (% BS) | nH |
|---|---|---|---|---|
| SUR1 | [3H]GBC | 120 (48,280) | 48±11 | 1.5±0.1 |
| SUR2A(YS) | [3H]GBC | 38 (29,50) | 82±11 | 1.0 |
| SUR2Aa | [3H]P1075 | 72 (52,100) | 88±8 | 1.0 |
| SUR2B | [3H]P1075 | 43 (28,65) | 87±4 | 1.0 |
A denotes the extent of inhibition (amplitude), nH the Hill coefficient. Parameters are derived from three to six inhibition curves.
a
At [DOGS-NTA]=3 μM, binding was stimulated to 107%.