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Setiptiline

Setiptiline
Setiptiline 2D structure.svg
Clinical data
Trade namesTecipul
SynonymsTeciptiline; delta(13b,4a),4a-Carba-mianserin; MO-8282; ORG-8282
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral
ATC code
  • none
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.055.123 Edit this at Wikidata
Chemical and physical data
FormulaC19H19N
Molar mass261.36 g/mol g·mol−1
3D model (JSmol)
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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

Setiptiline[3]
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,[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.

See also

References

  1. ^ 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.
  2. ^ Swiss Pharmaceutical Society, ed. (2000). Index Nominum 2000: International Drug Directory. Medpharm Scientific Publishers. p. 942. ISBN 3-88763-075-0.
  3. ^ 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.
  4. ^ 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. PMID 3792961.
  5. ^ 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. PMID 2881854.
  6. ^ 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.