TABLE 1

Comparison of [3H]repaglinide binding data on Kir6.2/SUR1 and Kir6.2/SUR1[S1237Y]

CompoundKir6.2/SUR1
Kir6.2/SUR1[S1237Y]
IC50 (nmol/l)nHKi (nmol/l)IC50 (nmol/l)nHKi (nmol/l)
Repaglinide1.9 ± 0.8−1.19 ± 0.100.6 ± 0.31.2 ± 0.7−1.05 ± 0.140.4 ± 0.2
Glibenclamide0.7 ± 0.2−1.14 ± 0.130.2 ± 0.1105 ± 17−0.90 ± 0.2536 ± 6
Nateglinide679 ± 121−0.98 ± 0.05235 ± 42>30,000N/AN/A
Tolbutamide26,000 ± 9,300−0.91 ± 0.129,000 ± 3,220>300,000N/AN/A
  • Data are means ± SD (n = 3). N/A, not applicable; nH, Hill coefficient.