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Aptazapine

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Aptazapine
Clinical data
ATC code
  • none
Identifiers
  • 2-methyl-1,3,4,14b-tetrahydro-2H,10H-pyrazino[1,2-a]pyrrolo[2,1-c][1,4]benzodiazepine
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC16H19N3
Molar mass253.349 g·mol−1
3D model (JSmol)
  • 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 checkY
  • Key:MNHDDERDSNZCCK-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Aptazapine (developmental code nameCGS-7525A) is atetracyclic antidepressant (TeCA) that was assayed inclinical trials for the treatment ofdepression in the 1980s but was never marketed.[1][2][3] It is apotentα2-adrenergic receptorantagonist with about 10 times the strength of the related compoundmianserin and has also been shown to act as a5-HT2 receptorantagonist andH1 receptorinverse agonist, while having no significant effects on thereuptake ofserotonin ornorepinephrine.[1][4] Based on its pharmacological profile, aptazapine may be classified as anoradrenergic and specific serotonergic antidepressant (NaSSA).

See also

[edit]

References

[edit]
  1. ^abLiebman 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

[edit]
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
Others
Non-selective
MAOATooltip Monoamine oxidase A-selective
MAOBTooltip Monoamine oxidase B-selective
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α1
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Classes
Antidepressants
(Tricyclic antidepressants(TCAs))
Antihistamines
Antipsychotics
Anticonvulsants
Anticholinergics
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