Table 1

Profiling of TM30089 at relevant 7TM receptors (binding or functional assays) and enzymes (enzymatic assays).

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


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.

Uller et al. Respiratory Research 2007 8:16   doi:10.1186/1465-9921-8-16

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