Phenylbiguanide-hydrochloride-N-Phenylbiguanide-hydrochloride-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPhenylbiguanidehydrochlorideCat.No.:HY-101331ACASNo.:55-57-2Synonyms:N-Phenylbiguanidehydrochloride;PBGhydrochloride;1-Phenylbiguanidehydrochloride分⼦式:C₈H₁₂ClN₅分⼦量:213.67作⽤靶点:5-HTReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Storeatroomtemperature3years*Insolvent:-80°C,6months;-20°C,1month(Storeatroom

temperature3years)BIOLOGICALACTIVITY⽣物活性Phenylbiguanidehydrochloride⼀种选择性的5-HT3受体激动剂，EC50为3.0±0.1μM。IC50&Target5-HT3Receptor3μM(EC50)体外研究Phenylbiguanide(1-Phenylbiguanide)isa5-HT3receptorselectiveagonistwithpEC50sof5.57,4.07,and4.47forr5-HT3A(b),h5-HT3A,m5-HT3A(b),respectively[1].TheeffectofPhenylbiguanide(1-Phenylbiguanidehydrochloride)inpromotingthegrowthoftheHT29celllineisinvestigated.PhenylbiguanidecausesadosedependentproliferationofHT29cellsafter48hoursincubation.Themaximumproliferationisata5HTconcentrationof12.5μM(P≤0.01).Phenylbiguanidesignificantlystimulatesthegrowthofcellsatconcentrationsof3.125μM(P≤0.05)and6.25μM(P≤0.01)[2].体内研究Inanaesthetisedmice,Phenylbiguanide(PBG),adrugthatisknowntostimulatecardiopulmonaryafferentC-fibres,isinjectedintotherightatriumoftheheartandmappedc-Fosexpressionwithinspecificregionsofthecentralnervoussystem.IntraatrialinjectionofPBGproducesareflexcardiorespiratoryresponseincludingapronouncedbradycardiaandarespiratorydepression[3].PROTOCOL1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellAssay[2]HT29cellsarewashedwithPhosphatebuffersaline(PBS)andharvestedwitha0.5%trypsinsolutionat50-60%confluency.Cellsarethenaddedtowellsatadensityof104cells/wellina96-wellplatetoafinalvolumeof100μL/well.After24hoursofincubationat37°Cina5%CO2atmosphere,theculturemediumisreplacedwith200μLfreshculturemediumcontaining5HThydrochloride,Phenylbiguanidehydrochlorideatconcentrationsof:3.125,6.25,12.5,25,50,and100µM.Cellsculturedsolelyinmediaservedasnegativecontrols.After48hoursofincubationat37°Cina5%CO2atmosphere,theculturemediumisremovedand8µLMTTreagent(dilutedinPBSataconcentrationof4mg/mL)isaddedto50μLoffreshculturemediumatafinalconcentrationof0.55mg/mL.Theoptimumincubationperiodtimeisdeterminedinapilotstudy[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[3]Administration[3]Adultmalespecifiedpathogenfree(SPF)BALB/cmice(28-33g;n=10)areusedthroughoutthisstudy.Allmicehavefreeaccesstowaterandfoodinalight(12:12hlight/darkcycle,lightsonat0700h)andtemperature-controlled(21-23°C)environment.Micearerandomlyassignedtotwotreatmentgroups,1)intra-atrialinjectionof0.9%saline(controls,n=5)or2)intra-atrialinjectionofvehiclecontainingPhenylbiguanide(n=5).ForthePBGinjectedgroup,miceareinjectedwithaneffectivedoseofPhenylbiguanide(1-1.5μgin10-15μLsaline).Thisisrepeatedfivetimesintotalwitheachinjectionseparatedby8-10min.Forcontrolmice,eachmousereceivesfivesalineinjections(10-15μLeach),alsoat8-10minintervals[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].MairID,etal.Pharmacologicalcharacterizationofarat5-hydroxytryptaminetype3receptorsubunit(r5-HT)expressedinXenopuslaevisoocytes.BrJPharmacol.1998Aug;124(8):1667-74.[2].AtaeeR,etal.Studyof5HT3andHT4receptorexpressioninHT29celllineandhumancolonadenocarcinomatissues.ArchIranMed.2010Mar;13(2):120-5.[3].deVriesA,etal.Characterisationofc-Fosexpressioninthecentralnervoussystemofmicefollowingrightatrialinjectionsofthe5-HT3receptoragonistPhenylbiguanide.AutonNeurosci.2005Dec30;123(1-2):62-75.McePdfHeig