Table 1 |
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|
Profiling of TM30089 at relevant 7TM receptors (binding or functional assays) and enzymes (enzymatic assays). |
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|
Receptor |
Assay typea |
% of controlb |
|
|
||
|
AT1 |
B |
90.1 ± 2.8 |
|
AT2 |
B |
98.1 ± 1.4 |
|
BLT1 |
B |
89.3 ± 3.5 |
|
C3a |
F |
88.7 ± 5.9 |
|
C5a |
B |
108.7 ± 6.3 |
|
ChemR23 |
F |
96.6 ± 1.6 |
|
CXCR2 |
B |
104.6 ± 6.1 |
|
CysLT1 |
B |
116.9 ± 10.5 |
|
Glucocorticoid |
B |
98.9 ± 11.3 |
|
Muscarinic (non-selective) |
B |
106.7 ± 8.5 |
|
Muscarinic (M2-selective) |
B |
97.5 ± 1.9 |
|
Phospholipase A2 |
E |
101.5 ± 1.0 |
|
COX1 |
E |
109.6 ± 3.6 |
|
COX2 |
E |
123.8 ± 13.4 |
|
iNOS |
E |
102.3 ± 3.6 |
|
|
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|
a Assay type: B – radioligand binding, F – functional InsP, and E – enzymatic assays. b Assays were performed in the absence (100% control) or presence of 10 μM TM30089 (% of control). Results are given as % of control ± SE (estimated) from 2–3 independent experiments. |
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|
Uller et al. Respiratory Research 2007 8:16 doi:10.1186/1465-9921-8-16 |
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