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Elzasonan

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Title: Elzasonan  
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Subject: GR-127935, RS-56812, 6-Chloro-5-ethoxy-N-(pyridin-2-yl)indoline-1-carboxamide, BRL-54443, SB-215505
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Elzasonan

Elzasonan
Systematic (IUPAC) name
4-(3,4-dichlorophenyl)-2-[2-(4-methylpiperazin-1-yl)-benzylidene]-thiomorpholin-3-one
Clinical data
Legal status
  • Uncontrolled
Routes Oral
Identifiers
CAS number  YesY
ATC code None
PubChem
UNII  YesY
Chemical data
Formula C22H23Cl2N3OS 
Mol. mass 448.4085 g/mol
 YesY   

Elzasonan (CP-448,187) is a selective 5-HT1B and 5-HT1D receptor antagonist that was under development by Pfizer for the treatment of depression but was discontinued, possibly due to poor efficacy.[1][2][3][4][5] By preferentially blocking 5-HT1B and 5-HT1D autoreceptors, elzasonan is thought to enhance serotonergic innervations originating from the raphe nucleus, thereby improving signaling to limbic regions like the hippocampus and prefrontal cortex and ultimately resulting in antidepressant effects.[3]

See also

References

  1. ^ José Miguel Vela; Helmut Buschmann; Jörg Holenz; Antonio Párraga; Antoni Torrens (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH.  
  2. ^ Stahl's essential psychopharmacology: neuroscientific basis and practical applications. Cambridge, UK: Cambridge University Press. 2008.  
  3. ^ a b "IngentaConnect 5-HT1 Receptor Augmentation Strategies as Enhanced Efficacy Thera...". 
  4. ^ "Pfizer, Inc.: analysis of patenting 1998 – 2001; Expert Opinion on Therapeutic Patents - 12(5):Pages 725-732 - Informa Healthcare". 
  5. ^ "Discontinued psychiatric drugs in 2008; Expert Opinion on Investigational Drugs - 18(10):Pages 1431-1443 - Informa Healthcare". 
5-HT1A agonists
GABAAR PAMs
α2δ VDCC blockers
Antidepressants
Sympatholytics
Others

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