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Adatanserin

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Title: Adatanserin  
Author: World Heritage Encyclopedia
Language: English
Subject: NBUMP, Flibanserin, 5-HT1A receptor, PNU-142633, E-55888
Collection: 5-Ht1A Agonists, 5-Ht2A Antagonists, 5-Ht2C Antagonists, Adamantanes, Carboxamides, Piperazines, Pyrimidines
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Adatanserin

Adatanserin
Systematic (IUPAC) name
N-[2-(4-pyrimidin-2-ylpiperazin-1-yl)ethyl]adamantane-1-carboxamide
Clinical data
Legal status
?
Identifiers
CAS number  N
ATC code None
PubChem
ChemSpider  YesY
UNII  YesY
ChEMBL  N
Chemical data
Formula C21H31N5O 
Mol. mass 369.50 g/mol
 N   

Adatanserin (WY-50,324, SEB-324) is a mixed 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2C receptor antagonist.[1][2][3] It was under development by Wyeth as an antidepressant but was ultimately not pursued.[3][4]

Adantaserin has been shown to be neuroprotective against ischemia-induced glutamatergic excitotoxicity, an effect which appears to be mediated by blockade of the 5-HT2A receptor.[5]

See also

References

  1. ^ Singh A, Lucki I (April 1993). "Antidepressant-like activity of compounds with varying efficacy at 5-HT1A receptors". Neuropharmacology 32 (4): 331–40.  
  2. ^ Kleven MS, Koek W (February 1996). "Pharmacological characterization of in vivo properties of putative mixed 5-HT1A agonist/5-HT2A/2C antagonist anxiolytics. I. Antipunishment effects in the pigeon". The Journal of Pharmacology and Experimental Therapeutics 276 (2): 388–97.  
  3. ^ a b Abou-Gharbia MA, Childers WE, Fletcher H, et al. (December 1999). "Synthesis and SAR of adatanserin: novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT(1A) and 5-HT(2) activity as potential anxiolytic and antidepressant agents". Journal of Medicinal Chemistry 42 (25): 5077–94.  
  4. ^ Stahl, S. M. (2000). Essential psychopharmacology: neuroscientific basis and practical application. Cambridge, UK: Cambridge University Press.  
  5. ^ Dawson LA, Galandak J, Djali S (March 2002). "Attenuation of ischemic efflux of endogenous amino acids by the novel 5-HT(1A)/5-HT(2) receptor ligand adatanserin". Neurochemistry International 40 (3): 203–9.  


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