Lesopitron

Chemical compound
  • none
Legal statusLegal status
  • In general: uncontrolled
Identifiers
  • 2-{4-[4-(4-chloro-1H-pyrazol-1-yl)butyl]piperazin-1-yl}pyrimidine
CAS Number
  • 132449-46-8
PubChem CID
  • 60813
ChemSpider
  • 54801
UNII
  • H1CGM4755H
CompTox Dashboard (EPA)
  • DTXSID40157587 Edit this at Wikidata
Chemical and physical dataFormulaC15H21ClN6Molar mass320.83 g·mol−13D model (JSmol)
  • Interactive image
  • 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).[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. ^ a b Micheli F (February 2001). "Lesopitron (Esteve)". IDrugs: The Investigational Drugs Journal. 4 (2): 218–24. PMID 16032484.
  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. doi:10.1345/aph.19041. PMID 10676820.
  • v
  • t
  • e
5-HT1ARTooltip 5-HT1A receptor agonistsGABAARTooltip GABAA receptor PAMsTooltip positive allosteric modulatorsHypnoticsGabapentinoids
(α2δ VDCC blockers)Antidepressants
AntipsychoticsSympatholytics
(Antiadrenergics)Others
  • v
  • t
  • e
SSRIsTooltip Selective serotonin reuptake inhibitors
SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors
NRIsTooltip Norepinephrine reuptake inhibitors
NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants
SARIsTooltip Serotonin antagonist and reuptake inhibitors
SMSTooltip Serotonin modulator and stimulators
Others
TCAsTooltip Tricyclic antidepressants
TeCAsTooltip Tetracyclic antidepressants
Others
Non-selective
MAOATooltip Monoamine oxidase A-selective
MAOBTooltip Monoamine oxidase B-selective
Miscellaneous
  • v
  • t
  • e
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins