Setiptiline
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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
| Site | Ki (nM) | Species | Ref |
|---|---|---|---|
| SERTTooltip Serotonin transporter | >10,000 (IC50) | Rat | |
| NETTooltip Norepinephrine transporter | 220 (IC50) | Rat | |
| DATTooltip Dopamine transporter | >10,000 (IC50) | Rat | |
| 5-HT1A | ND | ND | ND |
| 5-HT2A | ND | ND | ND |
| 5-HT2C | ND | ND | ND |
| α1 | ND | ND | ND |
| α2 | 24.3 (IC50) | Rat | |
| H1 | ND | ND | ND |
| mAChTooltip Muscarinic acetylcholine receptor | ND | ND | ND |
| 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,[citation needed] as well as an H1 receptor inverse agonist/antihistamine.[additional citation(s) needed]
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.