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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  |
| Chemical and physical data | |
| Formula | C19H19N |
| Molar mass | 261.368 g·mol−1 |
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Setiptiline (brand name Tecipul), also known as teciptiline, is a tetracyclic antidepressant (TeCA) which 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
| Site | Ki (nM) | Species | Ref |
|---|---|---|---|
| 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, 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
References
- ^ Buschmann, H.; Torrens, A.; Vela, J. M. (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. 1. Wiley VCH. p. 248. ISBN 978-3-527-31058-6.
- ^ Swiss Pharmaceutical Society, ed. (2000). Index Nominum 2000: International Drug Directory. Medpharm Scientific Publishers. p. 942. ISBN 3-88763-075-0.
- ^ Roth, BL; Driscol, J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
- ^ a b c d e Niho T, Ito C, Shibutani Y, Hashizume H, Yamaguchi K (1986). "[Pharmacological properties of MO-8282, a novel antidepressant]". Nippon Yakurigaku Zasshi (in Japanese). 88 (4): 309–20. doi:10.1254/fpj.88.309. PMID 3792961.
- ^ a b Mizota M, Oikawa Y, Nakayama K, Mizuguchi K, Takarada T, Kojima M, Kanehiro H, Funato H, Kayamoto M, Sato M (1986). "[Pharmacological studies of MO-8282, a new antidepressant]". Nippon Yakurigaku Zasshi (in Japanese). 88 (6): 457–66. doi:10.1254/fpj.88.457. PMID 2881854.
- ^ Przegaliński E, Baran L, Siwanowicz J, Rawłów A (1986). "The lack of antidepressant properties and a potent central antiserotonin activity of Org 8282". Pol J Pharmacol Pharm. 38 (4): 377–84. PMID 3774630.