Table 4.
ETBR signaling in response to ET‐1 and antagonist‐blocked ETAR. COS‐7 cells, expressing both ETBR and ETAR stimulated with either the non‐selective ET‐1 in the absence or presence of the ETAR‐selective antagonist sitaxentan. Ca2+ flux was monitored in duplicates and concentration‐response curved represent the average over all assay repetitions (n≥3).
|
Co‐transfection ratio |
|
Relative Ca2+ flux initiated by ETBR‐GFP |
||||||
|---|---|---|---|---|---|---|---|---|
|
|
ETBR expression |
ET‐1+vehicle |
ET‐1+sitaxentan |
|||||
|
|
[%] ±SEM |
EC50 [nM] |
pEC50 ±SEM |
[%] ±SEM |
EC50 [nM] |
pEC50 ±SEM |
[%] ±SEM |
|
|
ETBR/ETAR |
1 : 0 |
100±1 |
0.7 |
9.2±0.06 |
100±3 |
0.5 |
9.3±0.09 |
89±4 |
|
|
1 : 1 |
149±8 |
0.7 |
9.1±0.14 |
73±4 |
0.4 |
9.4±0.12 |
49±3 |