KI values for kinin analogs on WT B1 and B2 BK receptors and chimeric B1/B2 receptor constructs expressed in HEK293 cells
| Ligand | WTB1 | WTB2 | B2(B1ECIV) | B2(B1ECIV(N)) | B2(B1ECIV(C)) |
|---|---|---|---|---|---|
| nM4-a | |||||
| BK | 21700 ± 8700 | 1.92 ± 0.244-b | 793 ± 341 | 3.15 ± 1.84 | 22.4 ± 12.1 |
| L-Lys-BK | 441 ± 40 | 4.30 ± 0.274-b | 0.458 ± 0.006 | 1.06 ± 0.658 | 0.854 ± 0.363 |
| D-Lys-BK | 2820 ± 150 | 4.56 ± 0.55 | 121 ± 35 | ||
| Ala-BK | 12000 ± 4300 | 3.84 ± 0.17 | 414 ± 108 | ||
| Arg-BK | 1830 ± 180 | 7.14 ± 1.74 | 44.0 ± 5.0 | ||
↵4-a The constants are presented as K Ivalues. The values were calculated by the Radlig program with data obtained from competition-binding experiments with the agonists antagonists [3H]NPC17731 and [3H]desArg10[Leu9]-Lys-BK, and the values are presented as means ± S.E. of three experiments.
↵4-b From Fathy et al. (1998).