lesopitron

{{Short description|Chemical compound}}

{{Drugbox

| IUPAC_name = 2-{4-[4-(4-chloro-1H-pyrazol-1-yl)butyl]piperazin-1-yl}pyrimidine

| image = Lesopitron.png

| image_class = skin-invert-image

| tradename =

| pregnancy_category =

| legal_status = Uncontrolled

| routes_of_administration = Oral

| bioavailability =

| metabolism =

| elimination_half-life =

| excretion =

| CAS_number = 132449-46-8

| ATC_prefix = none

| ATC_suffix =

| PubChem = 60813

| ChemSpiderID = 54801

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = H1CGM4755H

| C=15 | H=21 | Cl=1 | N=6

| smiles = Clc1cn(nc1)CCCCN3CCN(c2ncccn2)CC3

}}

Lesopitron (E-4424) is a selective full agonist of the 5-HT_1A receptor which is structurally related to the azapirones.{{cite journal |vauthors=Haj-Dahmane S, Jolas T, Laporte AM, etal | title = Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat | journal = European Journal of Pharmacology | volume = 255 | issue = 1–3 | pages = 185–96 |date=April 1994 | pmid = 8026543 | doi = 10.1016/0014-2999(94)90097-3}} In 2001 it was under development by Esteve as an anxiolytic for the treatment of generalized anxiety disorder (GAD).{{cite journal | author = Micheli F | title = Lesopitron (Esteve) | journal = IDrugs: The Investigational Drugs Journal | volume = 4 | issue = 2 | pages = 218–24 |date=February 2001 | pmid = 16032484 }}{{cite journal | vauthors = Fresquet A, Sust M, Lloret A, etal | title = Efficacy and safety of lesopitron in outpatients with generalized anxiety disorder | journal = The Annals of Pharmacotherapy | volume = 34 | issue = 2 | pages = 147–53 | date = February 2000 | pmid = 10676820 | doi = 10.1345/aph.19041 | doi-access = }} It made it to phase II clinical trials but was apparently discontinued as no new information on lesopitron has surfaced since.