Aptazapine Explained

Aptazapine (developmental code name CGS-7525A) is a tetracyclic antidepressant (TeCA) that was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed.^{[1] [2] [3]} It is a potent α₂-adrenergic receptor antagonist with about 10 times the strength of the related compound mianserin and has also been shown to act as a 5-HT₂ receptor antagonist and H₁ receptor inverse agonist, while having no significant effects on the reuptake of serotonin or norepinephrine.^{[1] [4]} Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).

See also

• Mianserin
• Mirtazapine
• Setiptiline

Notes and References

1. Liebman JM, Lovell RA, Braunwalder A . CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist . Life Sciences . 32 . 4 . 355–63 . January 1983 . 6131367 . 10.1016/0024-3205(83)90081-4. etal.
2. Book: Author Unknown . Annual Reports in Medicinal Chemistry (Volume 20) . Academic Press . Boston . 1985 . 352 . 0-12-040520-2 .
3. Book: David J. Triggle . Dictionary of pharmacological agents . Chapman & Hall . London . 1997 . 0-412-46630-9 .
4. Gower AJ, Broekkamp CL, Rijk HW, Van Delft AM . Pharmacological evaluation of in vivo tests for alpha 2-adrenoceptor blockade in the central nervous system and the effects of the enantiomers of mianserin and its aza-analog ORG 3770 . Archives Internationales de Pharmacodynamie et de Thérapie . 291 . 185–201 . 1988 . 2896489 .