Table 2.
Radioligand displacement in tissue homogenate from mouse brain striatum ([3H]WIN 35428 at DAT) or hippocampus ([3H]Nisoxetine at NET & [3H]Citalopram at SERT).
| Compound Name | DAT [3H]WIN 35428 IC50 in μM [95% CI] (n) |
NET [3H]Nisoxetine IC50 in μM [95% CI] (n) |
SERT [3H]Citalopram IC50 in μM [95% CI] (n) |
|---|---|---|---|
|
Substrate: Dopamine (DAT) Dopamine (NET) Serotonin (SERT) |
99.8
aa [28.6 – 347.9] (5) |
12.7
aaa [8.2 – 20.2] (4) |
14.2 [4.1 – 49.2] (4) |
|
Inhibitor: WIN 35428 (DAT) Desipramine (NET) Citalopram (SERT) |
0.06
aaa, bbb [0.0.25 – 0.14] (3) |
0.01
aaa, bbb [0.005 – 0.002] (3) |
0.01
aaa, bbb [0.008 – 0.015] (4) |
| Decynium 22 |
10.8
bb [5.4 – 21.4] (4) |
100.7
bbb [34 – 245] (5) |
26.2 [16 – 42.9] (4) |
| Compound 1 |
20.9
b [11.8 – 36.8] (3) |
61.3
bb [24.1 – 134.1] (4) |
15.6 [7.3 – 33.2] (4) |
| Compound 2 |
15.0
b [6.8 – 33.2] (3) |
23.1 [8.1 – 74.3] (4) |
18.4 [14.6 – 23.3] (4) |
| Compound 3 |
30.9 [5.9 – 162.9] (2) |
18.0 [2.67 – 99.4] (4) |
10.3
aa [7.7 – 13.8] (4) |
| Compound 4 |
0.32
aaa, bbb [0.048 – 2.2] (3) |
11.9
aa [5.52 – 25.6] (4) |
1.04
aaa, bbb [0.75 – 1.46] (4) |
| Compound 5 |
223.8
a [0.21 – 0.24M] (3) |
31.9 [8.05 – 126.6] (5) |
13.9 [8.04 – 23.9] (4) |
| Compound 6 |
10.74
b [6.05 – 19.1] (3) |
55.5
b [10.9 – 282.5] (3) |
0.75
aaa, bbb [0.52 – 1.1] (3) |
| Compound 7 |
12.9
b [4.98 – 33.2] (3) |
222.9
bb [0.43– 0.11M] (3) |
1.14
aaa, bbb [0.84 – 1.5] (3) |
IC50 estimations determined from concentration response curves (Figs. 1–3) fit to a nonlinear regression.
a
P < 0.05
aa
P < 0.01
aaa
P < 0.001 indicates significance of difference for the compound versus decynium 22 (D22) within each radioligand.
b
P < 0.05
bb
P < 0.01
bbb
P < 0.001 denotes significant difference between the compound and reference transporter substrate, either dopamine (DAT and NET) or serotonin (SERT).