Table 1 Apparent potency values (pEC50) and pseudo-Hill slopes (nH) of norepinephrine (NE), dopamine (DA) and epinephrine (EP) in the absence (−) or presence of 1 µM nisoxetine on JumpIn-NET cells treated with vehicle (−dox) or doxycycline (+dox) in TRACT assays.

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

Substrate

 

Pretreatment

pEC50 ± SEMa,b

Slope (nH) ± SEMa,b

n

NE

 −dox

6.4 ± 0.1

0.8 ± 0.1

7

 −dox

Nisoxetine

6.5 ± 0.0

0.9 ± 0.1

5

 +dox

5.2 ± 0.1***

2.1 ± 0.2***

8

 +dox

Nisoxetine

6.3 ± 0.1d

0.9 ± 0.1d

6

DA

 −dox

5.1 ± 0.1

0.8 ± 0.1

3

 +dox

4.7 ± 0.0**

1.5 ± 0.1**

7

 +dox

Nisoxetine

4.4 ± 0.1c

0.6 ± 0.0d

4

EP

 −dox

6.4 ± 0.2

0.6 ± 0.0

3

 +dox

5.4 ± 0.1***

0.8 ± 0.1

6

 +dox

Nisoxetine

6.3 ± 0.1d

0.6 ± 0.1

3

  1. apEC50 values and pseudo-Hill slopes are reported as the mean ± SEM of three to eight individual experiments performed in duplicate.
  2. bSignificant difference between two mean potency values was determined by an unpaired two-tailed Student’s t-test. **p < 0.01, ***p < 0.001, compared to vehicle-treated (− dox) cells in the absence (–) of 1 µM nisoxetine using the same substrate. cp < 0.05, dp < 0.001, compared to doxycycline-treated (+dox) cells in the absence (–) of 1 µM nisoxetine using the same substrate.