Setiptiline (brand name Tecipul), also known as teciptiline, is a tetracyclic antidepressant (TeCA) that acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). It was launched in 1989 for the treatment of depression in Japan by Mochida.

Pharmacology

Pharmacodynamics

+ Setiptiline Site Ki (nM) Species Ref >10,000 (IC50) Rat 220 (IC50) Rat >10,000 (IC50) Rat 5-HT1A 5-HT2A 5-HT2C α1 α2 24.3 (IC50) Rat H1 Values are Ki (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site.

Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

Chemistry Setiptiline has a tetracyclic structure and is a close analogue of mianserin and mirtazapine, with setiptiline being delta(13b,4a),4a-carba-mianserin, and mirtazapine being 6-azamianserin.

See also Aptazapine Mianserin Mirtazapine

References