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Ex/Em(nm)	None/None
MW	N/A
CAS#	N/A
Solvent	N/A
Storage	N2(L)
Category	GPCR cAMPGPCRAssays
Related	BiochemicalAssays

Gproteincoupledreceptors(GPCR)areoneofthelargestreceptorclassestargetedbydrugdiscoveryprograms.Calciumflux(coupledviaGqpathway)assayisapreferredmethodindrugdiscoveryforscreeningGPCRtargets.However,over60%oftheknownGPCRssignalthroughadenylylcyclaseactivitycoupledtocAMP.MostoftheexistingcAMPassaysnotonlyrequirecelllysisbutalsolackbothtemporalandspatialresolution.ScreenQuest™LiveCellcAMPAssayServicePackprovidesthereal-timemonitoringofintracellularcAMPchangeinahigh-throughputformatwithoutacelllysisstep.Theassayworksthroughthecelllinesthatcontaineitheranexogenouscyclicnucleotide-gatedchannel(CNGC)orthepromiscuousG-protein,G?16.ThechannelisactivatedbyelevatedlevelsofintracellularcAMP,resultinginionfluxandcellmembranedepolarizationwhichcanbedetectedwitheitherafluorescentcalcium(suchasQuestFluo-8AM™)orafluorescentmembranepotentialdye.Co-expressionofG?16withspecificnon-Gq-coupledreceptorswillresultinthegenerationofanintracellularcalciumsignaluponreceptorstimulation.TheScreenQuest™LiveCellcAMPAssayServicePackprovidesbothcelllinesandreagentsforthemeasurementofintracellularcAMPchangeswithaFLIPR,aFDSSorotherequivalentfluorescencemicroplatereaders.IthasbeensuccessfullyusedtomeasureGsandGicoupledGPCRactivity.

References&Citations

CitationExplorer

ActivationofP2X7andP2Y11purinergicreceptorsinhibitsmigrationandnormalizestumor-derivedendothelialcellsviacAMPsignaling
Authors:DAvanzato,TGenova,AFiorioPla,MBernardini,SBianco,BBussolati,DMancardi,EGiraudo,FMaione,PCassoni
Journal:ScientificReports(2016)

TheM2muscarinicreceptorsareessentialforsignalingintheheartleftventricleduringrestraintstressinmice
Authors:HanaTomankova,PaulinaValuskova,EvaVarejkova,JanaRotkova,JanBenes,JaromirMyslivecek
Journal:Stress(2015)

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