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aptazapine

n. A tetracyclic antidepressant evaluated in the 1980s but never marketed.

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Aptazapine

Aptazapine (CGS-7525A) is a tetracyclic antidepressant (TeCA) which was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed. It is a potent α-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been shown to act as a 5-HT receptor antagonist and H receptor inverse agonist, while having no significant effects on the reuptake of serotonin or norepinephrine. Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).