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BioassayTestedEverylotistried&testedinarelevantBIOLOGicalassay.
OurBioassay
AlomoneLabs Orphenadrinehydrochloride inhibitscharbacol-inducedCa2+ signalingin M1muscarinicreceptorexpressingC6cells.ChangesinintracellularCa2+ weredetectedviachangesinFluo-3emissionfollowingapplication.A.Normalizedfluorescencebeforeandafterco-application(at20seconds,seearrow)of10µMcarbacholand0-100µM Orphenadrinehydrochloride (#O-101)asindicated.TheblankresponsetoPBSperfusionisingray.B.Inhibition(aspercentofcontrol)of10µMCarbacholevokedCa2+ rise,plottedagainstOrphenadrineconcentrations.
- 1.Brocks,D.R. etal. (1999) J.Pharm.Pharm.Sci. 2, 39.
- 2.Desaphy,J.F. etal. (2009) Pain 142, 225.
- 3.Kornhuber,J. etal. (1995) J.Neural.Transm.Gen.Sect. 102, 237.
- 4.Pubill,D. etal. (1999) J.Pharm.Pharmacol. 51, 307.
Thegroupofanticholinergicdrugsincludesbenztropine,biperiden,diphenhydramine,ethopropazine,orphenadrine,procyclidineandtrihexyphenidyl.OrphenadrineasthecitratesaltisusedforthetreatmentofParkinson’sdiseaseandinmusculoskeletaldisorders.Itisalsousedasananalgesic,althoughitsmechanismofactionisstillunknown1,2.Orphenadrinebindstoandmodulatestheactivityofmuscarinicreceptorsofratbrain,withIC50of0.37µM1.
OrphenadrineinhibitsNaVchannelsinaconcentration-,voltage-andfrequency-dependentmannerbybindingtothesamereceptorasthelocalanesthetics2.OrphenadrinewasreportedasaMuscarinicreceptorantagonist,H1histaminereceptorantagonist,musclerelaxant,andinhibitsthenoradrenergictransporterandblockstheNMDAreceptorionchannel3,4.
Orphenadrinehydrochloride(#O-101) isahighlypure,synthetic,andbiologicallyactivecompound.



