Setiptiline
Antidepressant drug From Wikipedia, the free encyclopedia
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.[1][2]
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Clinical data | |
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Trade names | Tecipul |
Other names | Teciptiline; delta(13b,4a),4a-Carba-mianserin; MO-8282; ORG-8282 |
AHFS/Drugs.com | International Drug Names |
Routes of administration | Oral |
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ECHA InfoCard | 100.055.123 |
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Formula | C19H19N |
Molar mass | 261.368 g·mol−1 |
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Pharmacology
Summarize
Perspective
Pharmacodynamics
Site | Ki (nM) | Species | Ref |
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SERT | >10,000 (IC50) | Rat | [4] |
NET | 220 (IC50) | Rat | [4] |
DAT | >10,000 (IC50) | Rat | [4] |
5-HT1A | ND | ND | ND |
5-HT2A | ND | ND | ND |
5-HT2C | ND | ND | ND |
α1 | ND | ND | ND |
α2 | 24.3 (IC50) | Rat | [5] |
H1 | ND | ND | ND |
mACh | 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,[4] α2-adrenergic receptor antagonist,[5] and serotonin receptor antagonist,[6] likely at the 5-HT2 subtypes,[citation needed] as well as an H1 receptor inverse agonist/antihistamine.[4][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.
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References
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