Aptazapine

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Aptazapine
Aptazapine.svg
Systematic (IUPAC) name
2-methyl-1,3,4,14b-tetrahydro-2H,10H-pyrazino[1,2-a]pyrrolo[2,1-c][1,4]benzodiazepine
Identifiers
CAS Number 71576-41-5 N
ATC code none
PubChem CID: 51355
ChemSpider 46513 YesY
UNII 240J927J1R YesY
KEGG D02972 YesY
ChEMBL CHEMBL336712 YesY
Chemical data
Formula C16H19N3
Molecular mass 253.34 g/mol
  • c42c(N3C(c1cccn1C2)CN(CC3)C)cccc4
  • InChI=1S/C16H19N3/c1-17-9-10-19-14-6-3-2-5-13(14)11-18-8-4-7-15(18)16(19)12-17/h2-8,16H,9-12H2,1H3 YesY
  • Key:MNHDDERDSNZCCK-UHFFFAOYSA-N YesY
 NYesY (what is this?)  (verify)

Aptazapine (CGS-7525A) is a tetracyclic antidepressant (TeCA) which was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed.[1][2][3] It is a potent α2-adrenergic receptor antagonist with ~10x the strength of the related compound mianserin and has also been shown to act as a 5-HT2 receptor antagonist and H1 receptor inverse agonist, while having no significant effects on the reuptake of serotonin or norepinephrine.[1][4] Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA).

See also

References

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