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Lesopitron

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Title: Lesopitron  
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Subject: Sunepitron, 5-HT1A receptor, PNU-142633, RS-56812, E-55888
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Lesopitron

Lesopitron
Systematic (IUPAC) name
2-{4-[4-(4-chloro-1H-pyrazol-1-yl)butyl]piperazin-1-yl}pyrimidine
Clinical data
Legal status
  • Uncontrolled
Routes Oral
Identifiers
CAS number
ATC code None
PubChem
ChemSpider
UNII  YesY
Chemical data
Formula C15H21ClN6 
Mol. mass 320.82 g/mol

Lesopitron (E-4424) is a selective full agonist of the 5-HT1A receptor which is structurally related to the azapirones.[1] In 2001 it was under development by Esteve as an anxiolytic for the treatment of generalized anxiety disorder (GAD).[2][3] It made it to phase II clinical trials but was apparently discontinued as no new information on lesopitron has surfaced since.[2][3]

See also

References

  1. ^ Haj-Dahmane S, Jolas T, Laporte AM, et al. (April 1994). "Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat". European Journal of Pharmacology 255 (1-3): 185–96.  
  2. ^ a b Micheli F (February 2001). "Lesopitron (Esteve)". IDrugs : the Investigational Drugs Journal 4 (2): 218–24.  
  3. ^ a b Fresquet A, Sust M, Lloret A, et al. (February 2000). "Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder". The Annals of Pharmacotherapy 34 (2): 147–53.  


5-HT1A agonists
GABAAR PAMs
α2δ VDCC blockers
Antidepressants
Sympatholytics
Others

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