Aptazapine

Chemical compound
  • none
Identifiers
  • 2-methyl-1,3,4,14b-tetrahydro-2H,10H-pyrazino[1,2-a]pyrrolo[2,1-c][1,4]benzodiazepine
CAS Number
  • 71576-40-4 ☒N
PubChem CID
  • 51355
ChemSpider
  • 46513 checkY
UNII
  • 240J927J1R
KEGG
  • D02972 checkY
ChEMBL
  • ChEMBL336712 checkY
Chemical and physical dataFormulaC16H19N3Molar mass253.349 g·mol−13D model (JSmol)
  • Interactive image
  • c42c(N3C(c1cccn1C2)CN(CC3)C)cccc4
InChI
  • 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 checkY
  • Key:MNHDDERDSNZCCK-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Aptazapine (developmental code name CGS-7525A) is a tetracyclic antidepressant (TeCA) that 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 about 10 times 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. 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. {{cite book}}: |author= has generic name (help)
  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.

External links

  • Media related to Aptazapine at Wikimedia Commons
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SSRIsTooltip Selective serotonin reuptake inhibitors
SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors
NRIsTooltip Norepinephrine reuptake inhibitors
NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants
SARIsTooltip Serotonin antagonist and reuptake inhibitors
SMSTooltip Serotonin modulator and stimulators
Others
TCAsTooltip Tricyclic antidepressants
TeCAsTooltip Tetracyclic antidepressants
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Non-selective
MAOATooltip Monoamine oxidase A-selective
MAOBTooltip Monoamine oxidase B-selective
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  • See also: Receptor/signaling modulators
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  • GSK1004723
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  • See also: Receptor/signaling modulators
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Antidepressants
(Tricyclic antidepressants (TCAs))
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