Setiptiline

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Setiptiline
Clinical data
Trade namesTecipul
Other namesTeciptiline; 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
  • 2-methyl-2,3,4,9-tetrahydro-1H-dibenzo[3,4:6,7]cyclohepta[1,2-c]pyridine
JSmol)
  • c42c(\C3=C(/c1ccccc1C2)CN(C)CC3)cccc4
  • InChI=1S/C19H19N/c1-20-11-10-18-16-8-4-2-6-14(16)12-15-7-3-5-9-17(15)19(18)13-20/h2-9H,10-13H2,1H3 checkY
  • Key:GVPIXRLYKVFFMK-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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 and Tetracyclic antidepressant § Binding profiles
Setiptiline[3]
Site Ki (nM) Species Ref
SERTTooltip Serotonin transporter >10,000 (IC50) Rat [4]
NETTooltip Norepinephrine transporter 220 (IC50) Rat [4]
DATTooltip Dopamine transporter >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
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

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. ISBN 978-3-527-31058-6.[permanent dead link
    ]
  2. 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. ^
    PMID 3792961
    .
  5. ^
    PMID 2881854
    .
  6. PMID 3774630
    .