grant
Novel Probes of the Kappa Opioid Receptor: Chemistry, Pharmacology, and Biology
Organization UNIVERSITY OF SOUTH FLORIDALocation TAMPA, UNITED STATESPosted 1 Jun 2011Deadline 28 Feb 2030
NIHUS FederalResearch GrantFY20263'5'-cyclic ester of AMPAdenosine Cyclic 3',5'-MonophosphateAdenosine Cyclic MonophosphateAdenosine, cyclic 3',5'-(hydrogen phosphate)Adverse effectsAffectAffective DisordersAffinityAgonistAnti-Anxiety AgentsAnti-Anxiety DrugsAnxietyAnxiolytic AgentsAnxiolyticsAssayAttributes of ChemicalsAzolesBehaviorBehavioralBindingBioassayBiological AssayBiologyBody TissuesBrainBrain Nervous SystemCell BodyCell Communication and SignalingCell LineCell SignalingCellLineCellsChemicalsChemistryChlorochinChloroquineChronicClinicalClinical TrialsCollectionCommon Rat StrainsComplexCorpus StriatumCorpus striatum structureCryo-electron MicroscopyCryoelectron MicroscopyCyclic AMPDarknessDevelopmentDihydrohydroxycodeinoneDiuresisDockingDopamineDrug KineticsDrug TargetingDrug abuseDrugsERK 1ERK1ERK1 KinaseElectron CryomicroscopyEncephalonExtracellular Signal-Regulated Kinase 1G Protein-Complex ReceptorG Protein-Coupled Receptor GenesG-Protein-Coupled ReceptorsG-ProteinsGPCRGTP-Binding ProteinsGTP-Regulatory ProteinsGoalsGuanine Nucleotide Coupling ProteinGuanine Nucleotide Regulatory ProteinsHemodialysesHemodialysisHumanHydroxytyramineHyperactivityIn VitroIn vivo analysisInfumorphIntermediary MetabolismIntracellular Communication and SignalingInvestigatorsItchingKO miceKadianKhingaminKnock-out MiceKnockout MiceLigandsLightLocomotor ActivityMAP Kinase 3MAPK3MAPK3 Mitogen-Activated Protein KinaseMAPK3 geneMS ContinMSirMeasuresMediatingMedicationMedicineMental DepressionMetabolic ProcessesMetabolismMiceMice MammalsMinor Tranquilizing AgentsMitogen-Activated Protein Kinase 3Mitogen-Activated Protein Kinase 3 GeneModelingModern ManMolecularMolecular InteractionMood DisordersMorphiaMorphineMotor ActivityMurineMusNerve CellsNerve UnitNeural CellNeurocyteNeurologicNeurologic ProcessNeurologicalNeuronsNociceptionNull MouseOpiate agonistOpiate receptor agonistOpiatesOpioidOpioid agonistOpioid receptor agonistOramorphOramorph SROverdoseOxycodeinonOxycodoneOxycodone SROxycontinP44ERK1PSTkinase p44mpkPainPainfulPharmaceutical PreparationsPharmacokineticsPharmacologyPhosphatesPhosphorylationPhotoradiationPhysiologicPhysiologicalPropertyProtein PhosphorylationPruritic DisorderPruritisPruritusRatRats MammalsRattusReceptor ActivationReceptor ProteinReceptor SignalingResearch PersonnelResearchersRodentRodentiaRodents MammalsRoxanolRoxicodoneSedation procedureSignal InductionSignal PathwaySignal TransductionSignal Transduction SystemsSignalingSignaling Factor Proto-OncogeneSignaling Pathway GeneSignaling ProteinStatex SRStrains Cell LinesStriate BodyStriatumStructural BiologistStructureStructure-Activity RelationshipTestingTherapeuticTherapeutic EffectTimeTissuesTransfectionTranslatingTreatment EfficacyWorkabuse of drugsabuses drugsaddictionaddictive disorderadenosine 3'5' monophosphateanti-depressant agentanti-depressant drugsanti-depressantsanti-depressive agentsantinociceptionantinociceptivebehavioral pharmacologybiological signal transductionbrain tissuecAMPchemical structure functionchemical synthesiscryo-EMcryoEMcryogenic electron microscopycultured cell linedepressiondevelopmentaldrug actiondrug/agentdysphoriahiPSChuman iPShuman iPSChuman induced pluripotent cellhuman induced pluripotent stem cellshuman inducible pluripotent stem cellshuman inducible stem cellsimprovedin vivoin vivo evaluationin vivo testinginduced human pluripotent stem cellsinnovateinnovationinnovativeinorganic phosphateinterdisciplinary approachintervention efficacyitch sensationkappa opiatekappa opioidkappa opioid receptorsmouse modelmultidisciplinary approachmurine modelneuronalnociceptivenon-human primatenonhuman primatenovelopiate use disorderopioid use disorderoxycodone self-administrationp44 MAPKpain reliefpharmacobehavioralpharmacologicpharmacophorepre-clinicalpreclinicalpreservationprogramsreceptorreceptor internalizationrecruitrelieve painresponsescaffoldscaffoldingsedationself-administer oxycodoneside effectstriatalstructure function relationshiptargeted drug therapytargeted drug treatmentstargeted therapeutictargeted therapeutic agentstargeted therapytargeted treatmenttherapeutic efficacytherapy efficacytoolκ opiateκ opioidκ opioid receptorsκ-ORκOR
Description preview
Project Summary
We propose to develop new kappa opioid receptor (KOR) agonists that have diverse signaling profiles with the
goal of correlating cellular signaling properties to favorable properties (antipruritic, anxiolytic and non-sedating)
in mice. The KOR is an attractive drug target because drugs that activate KOR do not lead to overdose or…
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