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工业互联网全球监测(2018年第十一期)_平台

苏州蚂蚁淘 /发布时间:1631554202 /浏览量:12

ProductDescription

PNU-282987isanα7nAChRagoNISTwithanEC50of154nMagainstthea7-5HT3chimera.Uptoconcentrationsof100uM,PNU-282987displayednoagonistactivityandnegligIBLeantagonisticactivity(60uM)towardtheneuromuscularjunctionformofthereceptorandtheganglionicnAChR(a3b4).PNU-282987isafunctionalantagonistofthe5-HT3receptoratanIC50of4.5uM.(1)

CotreatmentofPC12cellswithnAChRmodulatorPNU120596andPNU-282987significantlyinducesERK1/2phosphorylation.(2)Inachloralhydrate-anesthetizedratmodel,PNU-282987wasshowntorestoreamphetamine-inducedsensorygatingdeficitandmayhaveimplicationsinthetreatmentofschizophrenia.(3)

Technicalinformation:

ChemicalFormula:		C₁₄H₁₇ClN₂O
CAS#:		123464-89-1
MolecularWeight:		264.75
Purity:		>98%
Appearance:		white
ChemicalName:		N-(3R)-1-AzABIcyclo[2.2.2]oct-3-yl-4-chlorobenzamide
Solubility:		Upto100mMinDMSO
Synonyms:		PNU-282987,PNU282987,PNU282987

ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4^oCdesiccated,orstoreDMSOsolutionat-20^oC.

Reference:

1.	Bodnaretal.,DiscoveryandStructure-ActivityRelationshipofQuinuclidineBenzamidesasAgonistsofa7NicotinicAcetylcholineReceptors.J.Med.Chem.2005,48,905-908.PubmedID:15715459
2.	ElKouhenetal.,Pharmacologyofa7nicotinicacetylcholinereceptormediatedextracellularsignal-regulatedkinasesignallinginPC12cells.Br.J.Pharmacology,2009,156,638-648.PubmedID:19226255
3.	Hajosetal.,TheSelectivea7NicotinicAcetylcholineReceptorAgonistPNU-282987[N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-4-chlorobenzamideHydrochloride]EnhancesGABAergicSynapticActivityinBrainSlicesandRestoresAuditoryGatingDeficitsinAnesthetizedRats.J.Pharmcol.Exp.Ther.2005,312(3),1213-1222.PubmedID:15523001

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