Description
Clonidineisanα2-adrenergicreceptoragoNISTthatalsoactivatetheimidazoline1receptor,increasingdownstreamcatecholaminesynthesis.Clonidineexhibitsantihypertensive,neuromoduatory,cognitionenhancing,antinociceptive,analgesic,andantipsychoticactivities.Inhypertensiverats,clonidineincreasesbaroreceptorsensitivityanddecreasesbloodpressureandheartrate.Inotheranimalmodels,clonidineinhibitslongtermpotentiation(synapticplasticity)anddecreasesexcitatorypostsynapticpotentials(EPSPs)inthemedialprefrontalcortex(mPFC),apotentialmechanismbehindclonidine’sABIlitytodecreaseglutamaterelease.Clonidinealsoimprovesspatialmemoryimpairmentsinvivo.Thiscompoundisoccasionallyusedclinicallyforitsantipsychoticbenefitsandismostoftenusedtotreatattentiondeficithyperactivedisorder(ADHD)asaresultofitsactionsthatstemfrombindingpostsynapticα2-adrenergicreceptors.Invitro,clonidineinhibitsNav1.7Na+channels.Invivo,clonidinedecreasesmechanicalandthermalpaininamodelofchronicconstrictioninjury-inducedneuropathy,likelyduetoitsabilitytodownregulateexpressionofphosphorylatedNMDAreceptorsubunit1(pNR1).ClonidinealsodisplayssomesedativeactivityandinducesdownstreamactivationofhistamineH2receptors.