Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELuAF21934Cat.No.:HY-100366CASNo.:1445605-23-1分?式:C??H??Cl?N?O?分?量:315.2作?靶點:mGluR作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:≥80mg/mL(253.81mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1726mL15.8629mL31.7259mL5mM0.6345mL3.1726mL6.3452mL10mM0.3173mL1.5863mL3.1726mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(7.93mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.93mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.93mM);ClearsolutionBIOLOGICALACTIVITY?物活性LuAF21934選擇性和腦滲透性的mGlu4受體正變構調節劑，對mGlu4受體的EC50為500[1]。IC50&TargetmGlu4Receptor500nM(EC50)體內研究LuAF21934treatmentshowsadose-dependentanxiolytic-likeeffectinthestress-inducedhyperthermia,four-plate,andmarble-buryingtests.Theanti-hyperthermiceffectofLuAF21934(5mg/kg)intheSIHtestisinhibitedbythebenzodiazepinereceptorantagonistflumazenil(10mg/kg)andisnotserotonindependent.LuAF21934doesnotproduceantidepressant-likeeffectsinthetailsuspensiontestinmice;however,itdecreasesthebasallocomotoractivityofmicethatarenothabituatedtoactivitycages[1].LuAF21934(0.5-5mg/kgsc)doesnotinfluencetremorbutatdosesof0.5and2.5mg/kgreversesharmaline-inducedhyperactivity.LuAF21934atadoseof2.5mg/kgpotentiatestheinhibitoryinfluenceofharmalineontheexploratoryactivityandAP1duringthefirst30minofthemeasurementandcounteractstheharmaline-increasedbasicactivityduringtheperiodof30-90min[2].LuAF21934(0.1-5mg/kg)dose-dependentlyinhibitshyperactivityinducedbyMK-801oramphetamine.Italsoantagonizesheadtwitchesandincreasesfrequencyofspontaneousexcitatorypostsynapticcurrentsinbrainslices,inducedbyDOI[3].PROTOCOLAnimalRats:LuAF21934isdispersedin20%(2-hydropropyl)-b-cyclodextrinandareadministeredsubcutaneouslyAdministration[1](s.c.)60minbeforethetest.LuAF21934(2,5,10and15mg/kg,s.c.)anddiazepam(5mg/kg,i.p.)areadministeredacutely1hbeforetheVogel’sconflicttest.Theeffectsofeachdruginallexperimentsaremeasuredingroupsof8-10animals[1].Mice:LuAF21934isdispersedin20%(2-hydropropyl)-b-cyclodextrinandareadministeredsubcutaneously(s.c.)60minbeforethetest.Micearegentlyplacedintotheboxandallowedtoexplorefor15s.Then,eachtimeamousepassedfromoneplatetoanother,theexperimenterelectrifiesthewholefloorthusevokingavisibleflightreactionoftheanimal.Iftheanimalcontinuesrunning,nonewshockisdeliveredforthefollowing3s[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].AnnaS?awińska,etal.Anxiolytic-butnotantidepressant-likeactivityofLuAF21934,anovel,selectivepositiveallostericmodulatorofthemGlu?receptor.Neuropharmacology.2013Mar;66:225-35.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].OssowskaK,etal.LuAF21934,apositiveallostericmodulatorofmGlu4receptors,reducestheharmaline-inducedhyperactivitybutnottremorinrats.Neuropharmacology.2014Aug;83:28-35.[3].AnnaS?awińska,etal.Theantipsychotic-likeeffectsofpositiveallostericmodulatorsofmetabotropicglutamatemGlu4receptorsinrodents.BrJPharmacol.2013Aug;169(8):1824-39.McePdfHe