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Aptazapine

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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
Clinical data
Legal status
?
Identifiers
CAS number  N
ATC code None
PubChem
ChemSpider  YesY
UNII  YesY
KEGG  YesY
ChEMBL  YesY
Chemical data
Formula C16H19N3 
Mol. mass 253.34 g/mol
 N   

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. ^ a b 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.  
  2. ^ Author Unknown (1985). Annual Reports in Medicinal Chemistry (Volume 20). Boston: Academic Press. p. 352.  
  3. ^ David J. Triggle (1997). Dictionary of pharmacological agents. London: Chapman & Hall.  
  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.  


Receptor
(ligands)
H1
H2
H3
H4
Transporter
(blockers)
Enzyme
(inhibitors)
HDC
DAO
Others
Classes
Antidepressants
(TCAs and TeCAs)
Antihistamines
Antipsychotics
Anticonvulsants
Others
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