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- Wu,W. etal. (2012) Neurosci.Lett. 506, 307.
- AlomoneLabsAmitriptylinehydrochlorideinhibitsL-typevoltage-gatedCa2+ currentsexpressedin Xenopus oocytes.A.TimecourseofCaV1.2/α2-δ1/β1currentinhibitionby800µM Amitriptyline hydrochloride(#A-155).Currentswereelicitedbyapplicationofvoltagerampsfromaholdingpotentialof-100mVto+50mV(100msec).B.Superimposedexampletracesofcurrentresponsesbeforeandduringperfusionof800µMAmitriptylinehydrochloride,asindicated.
- 1.Soldatov,N.M. (2012) ISRNMol.Biol. 2012,691341.
- 2.Haderer,A. etal. (2003) Anesth.Analg. 96, 1707.
- 3.Baldessarini,R.J. etal.(1995) ThePharmacologicalBasisofTherapeutics 431.
- 4.Bryson,H.M.and Wilde,M.I. (1996) DrugsAging 8, 459.
- 5.Zahradník,I. etal.(2008) J.Pharmacol.Exp.Ther. 324, 977.
Voltage-gatedL-typeCaV1.2calciumchannelscouplemembranedepolarizationtotransientincreaseincytoplasmicfreeCa2+concentrationthatinitiatesanumberofessentialcellularfunctionsincludingcardiacandvascularmusclecontraction,geneexpression,neuronalplasticity,andexocytosis1.
Tricyclicantidepressants(TCAs)areknowntoinhibitCa2+currents,includingtheL-typeCaV1.2channelinheartmyocyteandneurons2.Otherknownphysiologicaltargetsoftricyclicantidepressantsinthecentralnervoussystemarethe5-HT2serotoninreceptorsandtheα1-adrenergicreceptors3.
Amitriptylinehydrochloride,atricyclicantidepressant,isusedforanumberofmedicalconditionsincludingmanagementofdepressive,anxietyandbipolardisorders3andmanagementofchronicpainsuchasneuropathicpain,diabeticneuropathy,postherpeticneuralgiaandfibromyalgia4.
Theproposedmechanismsofactionforamitriptylinehydrochlorideincludeinhibitionofthereuptakeofserotoninandnorepinephrine,inhibitionofNMDAreceptors,ofvoltage-gatedionchannelssuchasCa2+andNa+channelsandinteractionwithadenosinereceptors5.
Amitriptylinehydrochloride(#A-155) isahighlypure,synthetic,andbiologicallyactivecompound.