Pharmacological properties of diverse classes of antidepressant at constitutively active 5-HT2CINI receptors
The pKi values were determined by competition binding experiments using [3H]mesulergine as a radioligand. Isotherms were analyzed by nonlinear regression. The potencies of inverse agonists and neutral antagonists were evaluated upon basal (pEC50) and 5-HT-induced IP formation (pKb), respectively. All data are the mean ± S.E.M.s of three separate experiments each performed in triplicate.
Drug | Class | pKi | pKb | pEC50 | Action (PLC) |
|---|---|---|---|---|---|
| Mirtazapine | Tetracyclic | 8.22 ± 0.09 | 7.02 ± 0.17 | Inverse agonist | |
| Mianserin | Tetracyclic | 8.92 ± 0.04 | 7.74 ± 0.20 | Inverse agonist | |
| Clomipramine | Tricyclic | 7.53 ± 0.06 | 5.90 ± 0.03 | Neutral antagonist | |
| Amitriptyline | Tricyclic | 8.01 ± 0.13 | 7.06 ± 0.05 | Neutral antagonist | |
| Nefazodone | mCPP derivative | 7.37 ± 0.03 | 6.60 ± 0.04 | Neutral antagonist | |
| Trazodone | mCPP derivative | 6.81 ± 0.05 | 5.91 ± 0.09 | Neutral antagonist | |
| Fluoxetine | SSRI | 7.14 ± 0.07 | 5.70 ± 0.09 | Neutral antagonist | |
| Norfluoxetine | Fluoxetine metabolite | 7.01 ± 0.07 | 5.90 ± 0.05 | Neutral antagonist | |
| Citalopram | SSRI | 6.46 ± 0.22 | 5.83 ± 0.07 |
| Neutral antagonist |