Table 1 Effects of LUF6000 on the potency (-logEC50) and maximum effect (Emax) at the A3 AR of structurally diverse ligands measured with a [35S]GTPγS binding assay
Ligands | Emax (%) | -logEC50 (M) |
|---|---|---|
Cl-IB-MECA | 50.1 ± 2.4 | 7.52 ± 0.11 |
+LUF 0.1 μM | 60.4 ± 3.7 | 7.62 ± 0.12 |
+LUF 0.3 μM | 70.5 ± 5.2 | 7.54 ± 0.09 |
+LUF 1.0 μM | 82.4 ± 7.3 | 7.55 ± 0.10 |
+LUF 3.0 μM | 122 ± 3 | 7.20 ± 0.06 |
+LUF 10 μM | 125 ± 2 | 7.21 ± 0.06 |
NECA | 100 ± 3 | 6.79 ± 0.06 |
+LUF 1.0 μM | 119 ± 7 | 6.81 ± 0.10 |
+LUF 10 μM | 134 ± 5 | 6.61 ± 0.07 |
MRS541 | 24.3 ± 2.9 | 7.48 ± 0.31 |
+LUF 0.1 μM | 30.0 ± 1.7 | 7.43 ± 0.25 |
+LUF 0.3 μM | 45.0 ± 7.0 | 7.55 ± 0.22 |
+LUF 1.0 μM | 72.5 ± 7.6 | 7.39 ± 0.16 |
+LUF 3.0 μM | 116 ± 8 | 7.06 ± 0.11 |
+LUF 10 μM | 121 ± 6 | 6.99 ± 0.11 |
MRS542 | 5.6 ± 2.5 | NA |
+LUF 0.1 μM | 16.4 ± 3.1 | NA |
+LUF 0.3 μM | 34.2 ± 5.4 | 6.41 ± 0.47 |
+LUF 1.0 μM | 51.7 ± 4.1 | 7.12 ± 0.20 |
+LUF 3.0 μM | 69.2 ± 4.5 | 7.14 ± 0.15 |
+LUF 10 μM | 91.1 ± 4.1 | 6.82 ± 0.11 |
LUF5833 | 35.2 ± 5.2 | 6.02 ± 0.26 |
+LUF 0.1 μM | 63.8 ± 5.2 | 5.91 ± 0.14 |
+LUF 1.0 μM | 92.7 ± 9.7 | 5.92 ± 0.18 |
+LUF 10 μM | 102 ± 7.6 | 5.99 ± 0.13 |
MRS1220 | NA | NA |
+LUF 10 μM | NA | NA |