KD and K I values for BK and Lys-BK on the WT B1 and B2 BK receptors and chimeric B1/B2 receptor constructs expressed in HEK293 cells
| Construct | [3H] Agonist | [3H] Antagonist | ||||
|---|---|---|---|---|---|---|
| BK | Lys-BK | KD(BK)/KD(Lys-BK) | BK | Lys-BK | KI(BK)/KI(Lys-BK) | |
| nM3-a | ||||||
| WTB2 | 0.192 ± 0.0303-b | 0.157 ± 0.0073-b | 1.22 | 1.92 ± 0.243-b | 4.30 ± 0.273-b | 0.447 |
| WTB1 | 2880 ± 710 | 11.7 ± 1.33-c | 60.3 | 21700 ± 8700 | 441 ± 40 | 49.3 |
| B2(B1I;II;VII) | 0.580 ± 0.271 | 0.670 ± 0.010 | 0.866 | 0.547 ± 0.228 | 3.45 ± 1.77 | 0.166 |
| B2(B1IIIS111) | 0.566 ± 0.1493-b | 0.779 ± 0.1573-b | 0.727 | 137 ± 193-b | 117 ± 323-b | 1.17 |
| B2(B1IV) | 1.68 ± 1.16 | 3.01 ± 0.16 | 0.558 | 3.32 ± 0.74 | 8.34 ± 2.34 | 0.398 |
| B2(B1V) | 0.213 ± 0.064 | 0.417 ± 0.177 | 0.551 | 0.478 ± 0.475 | 4.41 ± 0.91 | 0.108 |
| B2(B1VIF259,T263) | 0.294 ± 0.111 | 0.148 ± 0.013 | 1.99 | 1.75 ± 0.043-c | 0.333 ± 0.0543-c | 5.26 |
| B2(B1ECI) | 4.10 ± 1.20 | 5.58 ± 2.60 | 0.735 | 38.6 ± 10.8 | 48.3 ± 19.2 | 0.799 |
| B2(B1ECII) | 0.547 ± 0.022 | 0.709 ± 0.071 | 0.772 | 0.807 ± 0.126 | 2.35 ± 0.148 | 0.343 |
| B2(B1ECIII) | 0.377 ± 0.030 | 0.315 ± 0.060 | 1.20 | 0.302 ± 0.221 | 3.16 ± 0.749 | 0.096 |
| B2(B1ECIV) | 2.63 ± 0.16 | 0.579 ± 0.177 | 4.54 | 793 ± 341 | 0.458 ± 0.006 | 1730 |
↵3-a The constants are presented as K D([3H] Agonist) and K I values ([3H] Antagonist). The values were calculated by the Radlig program with data obtained from hot and cold saturation-binding experiments and competition-binding experiments with the agonists [3H]BK and [3H]desArg10-Lys-BK and the antagonists [3H]NPC17731 and [3H]desArg10[Leu9]-Lys-BK, and the values are presented as means ± S.E. of three experiments.
↵3-b From Fathy et al. (1998).
↵3-c From Leeb et al. (1997).