Ratio of pharmacological affinity/activity for drug and metabolite against monoamine transporters Data were compiled from Sanchez and Hyttel (1999), Owens (1997), and Svartengren (1997).
Drug | Metabolite | Ratio of Activity of Metabolite to Parent Druga | ||||
|---|---|---|---|---|---|---|
| 5-HT | Noradrenaline | Dopamine | ||||
| Amitryptiline | Nortryptiline | 0.07 | 7 | Inactive | ||
| Dothiepin | Northiaden | 0.4 | 2.8 | Inactive | ||
| Dothiepin | Sulfoxide | Inactive | Inactive | Inactive | ||
| Imipramine | Desipramine | 0.06 | 31 | |||
| Imipramine | 2-Hydroxyimapramine | 1 | 1 | |||
| Clomipramine | Norcloipramine | 0.01 | 15 | |||
| Fluoxetine | Norfluoxetine | 1.8 | 0.64 | Inactive | ||
| Sibutramine | Desmethylsibutramine | 100 | 7 | |||
| Sibutramine | Didesmethylsibutramine | 100 | 6 | |||
| Sertraline | Desmethylsertraline | Inactive | Inactive | Inactive | ||
| Citaprolam | Desmethylcitalopram | 0.12 | Inactive | Inactive | ||
| Amperozide | FG5620 | Inactive |
|
| ||
↵ a This value is calculated as in vitro potency (e.g., Ki) of parent drug/in vitro potency of metabolite for the target receptor. The entry `inactive' means that the metabolite lacks appreciable affinity for the receptor