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Lesopitron

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
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
PubChemCID
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 aselectivefull agonist of the5-HT1A receptor which isstructurally related to theazapirones.[1] In 2001 it was under development byEsteve as ananxiolytic for the treatment ofgeneralized anxiety disorder (GAD).[2][3] It made it tophase IIclinical trials but was apparently discontinued as no new information on lesopitron has surfaced since.[2][3]

See also

[edit]

References

[edit]
  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. ^abMicheli F (February 2001). "Lesopitron (Esteve)".IDrugs: The Investigational Drugs Journal.4 (2):218–24.PMID 16032484.
  3. ^abFresquet 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.
5-HT1ARTooltip 5-HT1A receptoragonists
GABAARTooltip GABAA receptorPAMsTooltip positive allosteric modulators
Gabapentinoids
(α2δVDCCblockers)
Antidepressants
Sympatholytics
(Antiadrenergics)
Others
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
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
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