Aptazapine

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Aptazapine
File:Aptazapine.png
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
ATC code none
PubChem CID 51355
ChemSpider 46513
Chemical data
Formula C16H19N3
Molar mass 253.34 g/mol[[Script error: No such module "String".]]
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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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  2. Author Unknown (1985). Annual Reports in Medicinal Chemistry (Volume 20). Boston: Academic Press. p. 352. ISBN 0-12-040520-2. 
  3. David J. Triggle (1997). Dictionary of pharmacological agents. London: Chapman & Hall. ISBN 0-412-46630-9. 
  4. Gower AJ, Broekkamp CL, Rijk HW, Van Delft AM (1988). "Pharmacological evaluation of in vivo tests for alpha 2-adrenoceptor blockade in the central nervous system and the effects of the enantiomers of mianserin and its aza-analog ORG 3770". Archives Internationales De Pharmacodynamie Et De Thérapie. 291: 185–201. PMID 2896489.