Lesopitron

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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 132449-46-8
ATC code None
PubChem CID 60813
ChemSpider 54801
UNII H1CGM4755H 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. doi:10.1016/0014-2999(94)90097-3. PMID 8026543. 
  2. ↑ 2.0 2.1 Micheli F (February 2001). "Lesopitron (Esteve)". IDrugs : the Investigational Drugs Journal 4 (2): 218–24. PMID 16032484. 
  3. ↑ 3.0 3.1 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. PMID 10676820. 


Anxiolytics (N05B)
GABAA
PAMs
non-N05B
α2δ VDCC Blockers
5-HT1A Agonists
H1 Antagonists
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Antidepressants
Others

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc (eval/thrp), drug (N5A/5B/5C/6A/6B/6D)

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