The antidepressive effect of imipramine and its metabolite desipramine is most probably based on the inhibition of the re-uptake of noradrenaline and serotonin at the respective nerve endings. The effect on the serotoninergic system can be demonstrated with the serotonin uptake of the thrombocytes. Imipramine and desipramine also have a strong anticholinergic effect and serve as antagonists at H₁-receptors. Their effect on alpha-adrenoreceptors is limited.

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