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- Zheng,W. etal. (1991) Mol.Pharmacol. 40, 734.
AlomoneLabsFPL64176increasesL-typeCaV channelscurrentsexpressedin Xenopus oocytes.A.TimecourseofCaV1.2(coexpressedwithα2δ1andβ1auxiliarysubunits)tailpeakcurrentamplitude,elicitedby100msvoltagestepfromholdingpotentialof-100mVto-10mV,deliveredevery10seconds.Applicationof0.1and1µM FPL64176 (#F-160)increasestheCaV1.2current(indicatedbythehorizontalbar).B.Representativecurrenttracesbeforeandduringapplicationof0.1and1µMFPL64176(asindicated).
- 1.Zheng,W. etal. (1991) Mol.Pharmacol. 40, 734.
- 2.Ghais,N.S. etal. (2009) Exp.Physiol. 94, 240.
- 3.McDonough,S.I. etal. (2005) Biophys.J. 88, 211.
- 4.Fan,J.S. etal. (2002) Br.J.Pharmacol. 135, 1495.
- 5.Catterall,W.A. etal.(2003) Pharmacol.Rev. 55, 579.
FPL64176actsasanon-dihydropyridineL-typecalciumchannelactivatorwithhighefficacyproperties.It"sabenzoylpyrrolecompoundthathastheABIlitytoincreasemacroscopicinwardcurrentthroughL-typecalciumchannels.Itextendstheopeningofsinglecalciumchannelsduringdepolarizationandslowschannelclosinguponrepolarizationwithoutaffectingcurrentsthroughothercalciumchannels1-3.
FPL64176isbeingusedasatoolforstudyingthephysiologicalrolesanddisordersofL-typechannels,identificationofL-typecurrentswithinthemixofchannelsubtypesandforincreasingthecontractilityofsmoothandcardiacmuscle2.
TheuseofFPL64176hasrevealedaninactivationandadaptationprocessforryanodinereceptorsandthepresenceofcardiacsparklets3,4.
L-typevoltage-gatedcalciumchannelsareoneofthethreemajorclasses(CaV1-CaV3)ofvoltage-gatedcalciumchannels.Theyareexpressedinmanyexcitabletissuesandplayasimportanttransducersintheplasmamembrane,alteringmembranedepolarizationtointracellularsignaling.Manyphysiologicalfunctions,includingbrain,endocrine,andsensoryfunctionsandmusclecontractionrelyonproperL-typechannelactivity5.
FPL64176(#F-160)isahighlypure,synthetic,andbiologicallyactivecompound.



