Setiptiline

Antidepressant drug From Wikipedia, the free encyclopedia

Setiptiline

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]

Quick Facts Clinical data, Trade names ...
Setiptiline
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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
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
ECHA InfoCard100.055.123
Chemical and physical data
FormulaC19H19N
Molar mass261.368 g·mol−1
3D model (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 Y
  • Key:GVPIXRLYKVFFMK-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)
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Pharmacology

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Perspective

Pharmacodynamics

More information Site, Ki (nM) ...
Setiptiline[3]
SiteKi (nM)SpeciesRef
SERTTooltip Serotonin transporter>10,000 (IC50)Rat[4]
NETTooltip Norepinephrine transporter220 (IC50)Rat[4]
DATTooltip Dopamine transporter>10,000 (IC50)Rat[4]
5-HT1ANDNDND
5-HT2ANDNDND
5-HT2CNDNDND
α1NDNDND
α224.3 (IC50)Rat[5]
H1NDNDND
mAChTooltip Muscarinic acetylcholine receptorNDNDND
Values are Ki (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site.
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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

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