Table 1 Pharmacological properties of compounds 4a-c and 6a-b

From: A modular click ligand-directed approach to label endogenous dopamine D1 receptors in live cells

 

Functional

Binding (association-competition)

Binding (competition)

Compound

pKi ± SEM

RT ± SEM (min)

pKd ± SEM

pKi ± SEM

SKF83566

8.06 ± 0.10

5.6 ± 0.9

8.62 ± 0.14

8.71 ± 0.07

4a

7.38 ± 0.08

8.0 ± 1.2

8.10 ± 0.12

8.12 ± 0.11

4b

7.28 ± 0.17

5.0 ± 0.6

8.01 ± 0.08

8.13 ± 0.11

4c

7.20 ± 0.07

5.0 ± 1.0

7.94 ± 0.09

7.98 ± 0.07

6a

7.29 ± 0.21

7.5 ± 1.0

8.20 ± 0.10

8.20 ± 0.11

6b

6.36 ± 0.07

5.6 ± 1.2

7.26 ± 0.10

7.28 ± 0.12

  1. The inhibition of D1 functional activity by compounds 4a-c and 6a-b was assessed with a cell-based HTRF® cAMP Gs Dynamic assay with a constant 300 nM concentration of the agonist SKF38393. Cell-based Tag-Lite® association-competition binding assays were performed to obtain the kinetic binding properties of compounds 4a-c and 6a-b with F-ST-D1. With the same assay the corresponding pKi values were also obtained. Values are means of a minimum of 3 independent experiments with the corresponding standard error of the mean (SEM).
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