Article · Wikipedia archive · Last revised Jul 28, 2026

Lesopitron

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

Last revised
Jul 28, 2026
Read time
≈ 1 min
Length
176 w
Citations
5
Source
Wikipedia ↗
Lesopitron
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 2-{4-[4-(4-chloro-1H-pyrazol-1-yl)butyl]piperazin-1-yl}pyrimidine
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H21ClN6
Molar mass320.83 g·mol−1
3D model (JSmol)
  • Clc1cn(nc1)CCCCN3CCN(c2ncccn2)CC3

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).23 It made it to phase II clinical trials but was apparently discontinued as no new information on lesopitron has surfaced since.23

See also

See also

References

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. Micheli F (February 2001). "Lesopitron (Esteve)". IDrugs: The Investigational Drugs Journal. 4 (2): 218–24. PMID 16032484.
  3. 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. doi:10.1345/aph.19041. PMID 10676820.