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Setiptiline

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Setiptiline
Setiptiline 2D structure.svg
Clinical data
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
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 InfoCard 100.055.123
Chemical and physical data
Formula C19H19N
Molar mass 261.368 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 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.

Pharmacology

Pharmacodynamics

Setiptiline
Site Ki (nM) Species Ref
SERT >10,000 (IC50) Rat
NET 220 (IC50) Rat
DAT >10,000 (IC50) Rat
5-HT1A ND ND ND
5-HT2A ND ND ND
5-HT2C ND ND ND
α1 ND ND ND
α2 24.3 (IC50) Rat
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,α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

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



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