GTPγS | β-Arrestin | |||
---|---|---|---|---|
pEC50 | Efficacy | pEC50 | Efficacy | |
% | % | |||
Histamine | 6.2 ± 0.2 | 100 | 7.3 ± 0.1 | 100 |
Clobenpropit | 7.4 ± 0.2 | 84.1 ± 9.7 | 7.1 ± 0.1 | 86.2 ± 3.9 |
JNJ7777120 | −5.5 ± 2.8 | 7.9 ± 0.2 | 64.3 ± 5.1 | |
+ 300 nM Clobenpropit | 7.4 ± 0.1 | 68 ± 12.9 | ||
+ 1 μM Clobenpropit | 6.9 ± 0.2 | −6.0 ± 1.9 | ||
+ 10 μM Histamine | 5.6 ± 0.0 | 119 ± 0.0 | ||
Thioperamide | 8.0 ± 0.3 | −47.3 ± 4.1 | N.E. | N.E. |
+ 100 nM Histamine | 8.0 ± 0.02 | −6.7 ± 3.3 | ||
+ 100 nM JNJ7777120 | 6.4 ± 0.1 | −6.7 ± 2.4 | ||
+ 300 nM Clobenpropit | 6.3 ± 0.1 | −21.5 ± 1.1 | 7.6 ± 0.2 | −9.5 ± 1.3 |
N.E., no effect.