Table 2 Inhibitory potency (pIC50) values of NET inhibitors determined in the TRACT assay and fluorescent substrate uptake assay.

From: Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors

Inhibitor

pIC50a

TRACT assayb

n

Fluorescent substrate uptake assayc

n

Amitriptyline

6.7 ± 0.1

4

7.2 ± 0.1

5

Atomoxetine

7.7 ± 0.1

4

8.6 ± 0.0

3

Benztropine

6.5 ± 0.1

3

6.1 ± 0.1

3

Bupropion

4.9 ± 0.1

3

5.5 ± 0.0

3

Cocaine

6.2 ± 0.1

4

n.d.d

 

Desipramine

8.2 ± 0.1

3

8.6 ± 0.1

5

GBR12909

6.1 ± 0.2

3

6.0 ± 0.1

3

Maprotiline

7.3 ± 0.1

4

7.4 ± 0.1

3

Milnacipran

7.3 ± 0.2

4

7.8 ± 0.0

3

Nisoxetine

8.3 ± 0.1

7

8.4 ± 0.1

5

Nortriptyline

7.4 ± 0.1

5

8.0 ± 0.1

5

Reboxetine

8.3 ± 0.1

5

8.8 ± 0.0

5

  1. aThe mean pIC50 values found in the TRACT assay were on average 0.3 log-units lower than in the fluorescent substrate uptake assay (p = 0.016, paired two-tailed Student’s t-test).
  2. bIn the TRACT assay, values are reported as the mean ± SEM of three to seven individual experiments performed in duplicate.
  3. cIn the fluorescent substrate uptake assay the values are reported as the mean ± SEM of three to five individual experiments each performed in quadruplicate.
  4. dNot determined.