Aptazapine

Aptazapine
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
Molar mass 253.34 g/mol
 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

  1. 1 2 Liebman JM, Lovell RA, Braunwalder A; et al. (January 1983). "CGS 7525A, a new, centrally active alpha 2 adrenoceptor antagonist". Life Sciences 32 (4): 355–63. doi:10.1016/0024-3205(83)90081-4. PMID 6131367.
  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.
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