Aptazapine

In this article, we will explore the topic of Aptazapine in depth, analyzing its different facets and relevant aspects. From its origin and evolution to its impact on today's society, we will delve into history and its importance in different contexts. Additionally, we will examine the opinions and perspectives of experts in the field, as well as the experiences of those who have been directly affected by Aptazapine. Through a broad and multidisciplinary approach, we aim to shed light on this very relevant topic, offering the reader a complete and enriching vision.

Aptazapine
Clinical data
ATC code
  • none
Identifiers
  • 2-methyl-1,3,4,14b-tetrahydro-2H,10H-pyrazinopyrrolobenzodiazepine
CAS Number
PubChem CID
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 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.