Drug intelligence / Profile preview

aptazapine

Development stage
Discontinued
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Aptazapine is a tetracyclic antidepressant that was investigated as a potential treatment for depression. It is structurally and pharmacologically related to mirtazapine, another tetracyclic antidepressant, but was never marketed. Aptazapine acts primarily by antagonizing central presynaptic α2-adrenergic inhibitory autoreceptors and heteroreceptors, which increases central noradrenergic and serotonergic activity. It also antagonizes serotonin 5-HT2 and 5-HT3 receptors, histamine H1 receptors (contributing to sedative effects), peripheral α1-adrenergic receptors (which may cause orthostatic hypotension), and has moderate antimuscarinic activity. Despite its development as an antidepressant, it did not reach the market.

02

Targets

HTR3A (5-hydroxytryptamine receptor 3A)HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)ADRA2A (α2A)HRH1 (Histamine H1 Receptor)

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