Inhibition of [3H]glibenclamide binding to SUR subtypes by sulfonylureas and glinides (insulinotropes)
Inhibition curves were measured as shown in Fig. 3. pKi values are means ± S.E.M. of three to five individual experiments evaluated independently.
Insulinotrope | SUR Subsite(s) | Compound Number | pKi | ||||
|---|---|---|---|---|---|---|---|
| SUR1 | SUR2A(YS) | SUR2B(YS) | |||||
| Glibenclamide | A+B | 1 | 8.84 ± 0.02 | 8.30 ± 0.03 | 8.18 ± 0.05 | ||
| Glimepiride | A+B | 2 | 8.67 ± 0.03 | 7.93 ± 0.10 | 7.93 ± 0.05 | ||
| Gliquidone | A+B | 3 | 8.05 ± 0.03 | 7.40 ± 0.06 | 7.25 ± 0.03 | ||
| Gliclazide | A | 4 | 5.87 ± 0.04 | 5.39 ± 0.05 | 5.31 ± 0.02 | ||
| Glibornuride | A | 5 | 5.80 ± 0.07 | 5.33 ± 0.01 | 5.31 ± 0.09 | ||
| Nateglinide | A | 6 | 5.98 ± 0.03 | 5.61 ± 0.02 | 5.43 ± 0.08 | ||
| Meglitinide | B | 7 | 4.75 ± 0.03 | 4.70 ± 0.04 | 5.04 ± 0.03 | ||
| UL-DF 9 | B | 8 | 3.95 ± 0.04 | 4.41 ± 0.07 | 4.62 ± 0.05 | ||
| Repaglinide | B | 9 | 7.04 ± 0.04 | 7.33 ± 0.06 | 7.30 ± 0.06 | ||
| AZ-DF 265 | B | 10 | 5.86 ± 0.03 | 5.90 ± 0.05 | 5.89 ± 0.06 | ||