Aptazapine

Aptazapine

Aptazapine is a tetracyclic antidepressant (TeCA) that was developed in the late 1970s but was never marketed. It is structurally related to mianserin and mirtazapine and has similar effects, acting as an antagonist at H1 receptors, alpha-2 adrenergic receptors, and serotonin 5-HT2 receptors, and as an inverse agonist at serotonin 5-HT2C receptors.

Pharmacology

Aptazapine is a potent antihistamine, with this action likely underpinning its sedative effects. It is also a potent alpha-2 adrenoceptor antagonist, which likely confers some of its antidepressant effects. However, unlike mianserin and mirtazapine, aptazapine is a potent antagonist at serotonin 5-HT2A receptors, which may contribute to its different profile of effects.

Clinical Use

Despite its development, aptazapine was never marketed. It is not currently used in clinical practice. However, its pharmacological profile suggests that it may have potential uses in the treatment of depression, anxiety, and insomnia.

See Also

• Tetracyclic antidepressant
• Mianserin
• Mirtazapine

References

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