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1、0026-895X/90/050610-04$03.OO/OCopyrightbyTheAmericanSocietyforPharmacologyandExperimentalTherapeuticsAllrightsofreproductioninanyformreserved.MOLECULARPHARMACOLOGY,38:610-613ACCELERATEDCOMMUNICATIONIdentificationofTwoH3-HistamineReceptorSubtypesROBERTE.WEST,JR.,ADAMZWEIG,
2、NENG-YANGSHIH,MARVINI.SIEGEL,ROBERTW.EGAN,andMIKEA.CLARKDepartmentsofAllergyandImmunology(R.E.W.,AZ.,MIS.,R.W.E.,M.A.C.)andChemica!Research(N.V.S.),Schering-PloughResearch,Bloomfield,NewJersey07003ReceivedApril11,1990;AcceptedAugust27,1990DownloadedfromSUMMARYTheH3-histami
3、nereceptorprovidesfeedbackinhibitionofhista-ofprotein;K8=68nM,B,8=48fmol/mgofprotein.)Bun-minesynthesisandreleaseaswellasinhibitionofotherneuro-mamide,anotherantagonistthat,likethioperamide,containsatransmitterrelease.Wehavecharacterizedthisreceptorthioureabygroup,likewis
4、ediscriminatedbetweentwoclassesofradioligandbindingstudieswiththeH3agonistN’-[3H]methylhis-sites.Inadditiontodifferencesbetweensomeantagonistpoten-molpharm.aspetjournals.orgtamine([3H]NAMHA).Theresultsof[3H]NAMHAsaturationbind-ciesforthetworeceptors,thereisadifferentialgua
5、ninenucleo-ingandNAMHAinhibitionof[3HJNAMHAbindingwereconsistenttidesensitivityofthetwo.TheaffinityoftheH3Areceptorfor[3H]withanapparentlysingleclassofreceptors(K0=0.37flM,B,NAMHAwasreducedlessthan2-fold,whereas[3H]NAMHA=73fmol/mgofprotein)andcompetitionassayswithotherbin
6、dingtotheH3Breceptorwasundetectableinthepresenceofagonistsandtheantagonistsimpromidineanddimapritdisclosedguanosine5’-O-(3-thiotriphosphate).ThedistinctionbetweenH3Aonlyasingleclassofsites.Incontrast,inhibitionof[3H]NAMHAandH36receptorsubtypes,theformerahighaffinityandtheb
7、indingbythespecifichighaffinityH3antagonistthioperamidelatteralowaffinitythioperamidesite,drawssupportfrompub-revealedtwoclassesofsites(K,A=5nM,BrnaxA30ffllol/mgIishedinvitrodata.atRuthLillyMedicalLibraryonJuly4,2013TheH3-histaminereceptorisahighaffinityreceptorreportedDeb
8、riswassedimentedby10mmofcentrifugationat1000xg,aftertoinhibitcentralnervoussystemhistamin
