Table 2.
Inhibition of radioligand binding to SUR1 and SUR2 by OCoA
| SUR | Radioligand | MgATP (mM) | IC50 (μM) | nH |
|---|---|---|---|---|
| SUR1 | [3H]GBC | 0 | 6.1 (3.6,10) | 1.1±0.2 |
| SUR1 | [3H]GBC | 0.3 | 15 (12,18) | 2.1±0.2 |
| SUR2A(YS)a | [3H]GBC | 0.3 | 44 (25,60) | 1.2±0.2 |
| SUR2A | [3H]P1075 | 0.3 | 17 (15,21) | 1.5±0.1 |
| SUR2A/Kir6.2 | [3H]P1075 | 0.3 | 30 (27,32) | 1.4±0.1 |
| SUR2B | [3H]P1075 | 0.3 | 12 (7,20) | 1.8±0.2 |
Parameters are derived from experiments as shown in Figure 3. IC50 values are followed by the 95% confidence interval; nH denotes the Hill coefficient. In all cases, the inhibition curve reached completion.
a
At [OCoA]⩽1 μM, binding was stimulated to ∼110%.