Setiptiline Explained

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]}

Pharmacology

Pharmacodynamics

See also: Pharmacology of antidepressants.

Setiptiline^[3]

Site	Ki (nM)	Species	Ref
	>10,000 (IC50)	Rat	^[4]
	220 (IC50)	Rat
	>10,000 (IC50)	Rat
α2	24.3 (IC50)	Rat	^[5]
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,^[6] likely at the 5-HT₂ subtypes, as well as an H₁ receptor inverse agonist/antihistamine.^[4]

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

Notes and References

1. Book: Holenz J, Díaz JL, Buschmann H . Chemistry: Tricyclic and tetracyclic antidepressants . 10.1002/9783527619337.ch5 . Buschmann H, Torrens A, Vela JM . https://books.google.com/books?id=yXD4QA-Y_Z0C&pg=PA248 . Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application . 1 . 248 . Wiley VCH . 2007 . 978-3-527-31058-6 .
2. Book: Index Nominum 2000: International Drug Directory . 942 . Swiss Pharmaceutical Society . Medpharm Scientific Publishers . 2000 . 3-88763-075-0 .
3. Web site: PDSP K_i Database . Psychoactive Drug Screening Program (PDSP). Bryan Roth . Roth BL, Driscol J . University of North Carolina at Chapel Hill and the United States National Institute of Mental Health . 14 August 2017 .
4. Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K . [Pharmacological properties of MO-8282, a novel antidepressant] . ja . Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica . 88 . 4 . 309–320 . October 1986 . 3792961 . 10.1254/fpj.88.309 . free .
5. Mizota M, Oikawa Y, Nakayama K, Mizuguchi K, Takarada T, Kojima M, Kanehiro H, Funato H, Kayamoto M, Sato M . 6 . [Pharmacological studies of MO-8282, a new antidepressant] . ja . Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica . 88 . 6 . 457–466 . December 1986 . 2881854 . 10.1254/fpj.88.457 . free .
6. Przegaliński E, Baran L, Siwanowicz J, Rawłów A . The lack of antidepressant properties and a potent central antiserotonin activity of Org 8282 . Polish Journal of Pharmacology and Pharmacy . 38 . 4 . 377–384 . 1986 . 3774630 .