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Hello Bio/SR 95531 hydrobromide (Gabazine)/HB0901/50mg
Productoverview
- NameSR95531hydrobromide(Gabazine)
- ShortdescriptionSelective,competitiveGABAAreceptorantagoNIST
- BIOLOGicaldescription
SelectiveandcompetitiveGABAAreceptorantagonist(Ki=150nMfordisplacementof[3H]-GABAfromratmembranes).
DisplacesGABAfromtheGABAARagonistbindingsitetopreventreceptoractivation.AlsoactsasanegativeallostericinhibitorofchannelopeningtoinhibitGABAAreceptoractivationbyanaestheticagents.
InhibitsGABA-inducedCl-currentstoreduceGABA-mediatedsynapticinhibition.
Alsodisplayslowaffinityglycinereceptorinhibition.
Showsconvulsiveactions. - AlternativenamesGabazine|GBZ
- BiologicalactionAntagonist
- Purity>98%
- Customercomments
WeregularlyuseHelloBioGabazine(SR95531)inthelab.Weespeciallyliketheformulationwhereyouonlyneedtoadd1mlofwatertomakea10mMstocksolution.Verifiedcustomer,TheUniversityofNewcastle
Iamsatisfiedwiththequality,quickdeliveryandfollow-upofyourproduct.Verifiedcustomer,ShimaneUniversity
WeusedourfirstaliquotofSR95531(Gabazine)lastweek.TheexperimentwasacriticaloneforusandtheSR95531workedexactlyasexpected–100%blockofaGABAergicIPSP(inhibitorypostsynapticpotential).Verifiedcustomer,UniversityofMichigan
- Ourproductsinaction5citationsSubmitYourCitationNow
Images
Properties
- Chemicalname6-Imino-3-(4-methoxyphenyl)-1(6H)-pyridaziNEButanoicacidhydrobromide
- MolecularWeight368.23
- Chemicalstructure
- MolecularFormulaC15H17N3O3.HBr
- CASNumber104104-50-9
- PubChemidentifier107895
- SMILESCOC1=CC=C(C=C1)C2=NN(C(=N)C=C2)CCCC(=O)O.Br
- SourceSynthetic
- InChiInChI=1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H
- InChiKeyGFZHNFOGCMEYTA-UHFFFAOYSA-N
- MDLnumberMFCD00055135
- AppearanceWhitesolid
Applications
- Applicationnotes
Gabazine(SR95531)iscommonlyusedtoreducelevelsofinhibitionbyantagonisingGABAAreceptors.Itiscommonlyusedatconcentrationsbetween10–200μM.
Gabazine(SR95531)fromHelloBioblocksspontaneousinhibitorypostsynapticcurrents(IPSC)andevokedIPSCs(seeFig1above).Itwaseffectiveat1μMandcompletelyblockedGABAAreceptorsat20μM.
#Protocol1:Evokedandspontaneousinhibitorypostsynapticcurrents(IPSCs)
- WholecellvoltageclamprecordingswereobtainedfromlayerVneuronsofthemouseprelimbiccortexbrainslice.
- AstimulatingelectrodewasplacedinlayersII/IIIandIPSCswereevokedbyasinglesquare(150μs)pulseevery10secatastimulusintensitythatgaveareliableIPSC.
- IPSCswereevokedatarangeofneuronholdingvoltagestomeasurethereversalpotentialofthecurrenttoensureitwasGABAergic.
- Neuronswereheldat0mVandIPSCscontinuouslystimulatedandrecordedinresponseto5minapplicationsofvaryingconcentrationsofGabazineuntilcompletereceptorinhibition.
- SpontaneousIPSCswererecordedbeforeandafteradditionofGabazinebyholdingtheneuronat0mVandrecordingfor10sec.
- AllrecordingsforIPSCsweremadeinthepresenceofAMPARantagonists.
StoringandUsingYourProduct
- StorageinstructionsRoomtemperature
- SolubilityoverviewSolubleinwater(25mM)andinDMSO(100mM)
- ImportantThisproductisforRESEARCHUSEONLYandisnotintendedfortherapeuticordiagnosticuse.Notforhumanorveterinaryuse.
ReferencesforSR95531hydrobromide(Gabazine)
Biochemicalcharacterizationoftheinteractionofthreepyridazinyl-GABAderivativeswiththeGABAAreceptorsite.
HeaulmeMetal(1986)BrainRes384(2):224-31.PubMedID:3022866Sequentialstepsunderlyingneuronalplasticityinducedbyatransientexposuretogabazine.
PegoraroSetal(2010)JCellPhysiol222(3):713-28.PubMedID:20027606Thekineticsofinhibitionofratrecombinantheteromericalpha1betaglycinereceptorsbythelow-affinityantagonistSR-95531.
BeatoMetal(2007)JPhysiol580(Pt1):171-9.PubMedID:17218350ThedifferentialantagonismbybicucullineandSR95531ofpentobarbitone-inducedcurrentsinculturedhippocampalneurons.
UchidaIetal(1996)EurJPharmacol307(1):89-96.PubMedID:8831109TonicallyactivatedGABAAreceptorsinhippocampalneuronsarehigh-affinity,low-conductancesensorsforextracellularGABA.
Yeungetal(2003)MolPharmacol36(1):2-8.PubMedID:12488530