Evaluation of antidepressant compounds from distinct classes for antagonism of the AaDOP2 receptor
The effect of various concentrations of antidepressant compounds was tested for inhibition of 3 µM dopamine-stimulated cAMP in HEK-AaDOP2 receptor cells. Data represent the mean ± S.E.M. IC50 values for at least three independent experiments.
| Compound | IC50 ± S.E.M. | Chemical Class |
|---|---|---|
| nM | ||
| (+)-Butaclamol | 260 ± 32 | DR antagonist |
| Amitriptyline | 5.1 ± 1.2 | TCA |
| Amoxapine | 20 ± 8.4 | TeCA |
| Atomoxetine | No inhibitiona | NRI |
| Clomipramine | 56 ± 18 | TCA |
| Desipramine | 3300 ± 600 | TCA |
| Doxepin | 20 ± 6.2 | TCA |
| Fluoxetine | No inhibitiona | SSRI |
| Fluvoxamine | No inhibitiona | SSRI |
| Imipramine | 360 ± 34 | TCA |
| Norclomipramine | 670 ± 35 | TCA |
| Nortriptyline | 140 ± 50 | TCA |
| Protriptyline | 600 ± 250 | TCA |
| SCH-23390 | 1300 ± 340 | D1DR antagonist |
| Trazodone | No inhibitiona | SARI |
| Venlafaxine | No inhibitiona | SNRI |
D1DR, selective D1-like dopamine receptor antagonist; DR antagonist, nonselective dopamine receptor antagonist; NRI, norepinephrine reuptake inhibitor; SARI, serotonin antagonist and reuptake inhibitor; SNRI, serotonin and norepinephrine reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor; TCA, tricyclic antidepressant; TeCA, tetracyclic antidepressant.
↵a Less than 10% inhibition at 3 µM compound.