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- Olianas,M.C. etal. (2000)Br.J.Pharmacol. 131, 447.
AlomoneLabsMuscarinicToxin7inhibitsCarbachol-evoked[Ca2+]inincreaseinM1R-expressingC6cells.CellswereloadedwithFluo-3AMandpre-incubatedfor20minwithcontrolorwith25nMand100nMMuscarinicToxin7(#STM-200),asindicated,andstimulatedwith100µMCarbachol(arrow).ChangesinintracellularCa2+weredetectedaschangesinFluo-3emissionfollowingstimulation.
- 1.Felder,C.C. etal.(2000) J.Med.Chem. 43,4333.
- 2.Forsythe,S.M. etal.(2002) Am.J.Respir.Cell.Mol.Biol. 26,298.
- 3.Ferreira,A.R. etal.(2003) Pharmacol.Biochem.Behav. 74,411.
- 4.VanderZee,E.A. etal.(1999) Prog.Neurol. 58,409.
- 5.Adem,A.andKarlsson,E.(1997)LifeSci. 60, 1069.
- 6.Olianas,M.C. etal. (2000)Br.J.Pharmacol. 131, 447.
- 7.Kukkonen,A. etal. (2004)J.Biol.Chem. 279, 50923.
Theactionoftheneurotransmitteracetylcholine(Ach)ismediatedthroughtwotypesofreceptors,theionotropicnicotinicreceptorsandthemetabotropicmuscarinicreceptors.ThemuscarinicreceptorsbelongtothesuperfamilyofG-proteincoupledreceptors.Fivesubtypesofmuscarinicreceptorshavebeencloned:m1-m51,2.
Themuscarinicreceptorsarewidelydistributedthroughoutthebody,butarepredominantlyexpressedwithintheparasympatheticnervoussystemandexertbothexcitatoryandinhibitorycontrolovercentralandperipheraltissues1,2.
Muscarinicreceptorsparticipateinanumberofphysiologicalfunctionssuchasregulationofheartrate,musclecontraction,cognition,sensoryprocessingandmotorcontrol1.Theyalsoparticipateinlearningandmemoryprocessing3,4.
MuscarinicToxin7isa65aminoacidpeptidetoxinisolatedfromthe Dendroaspisangusticeps (Easterngreenmamba)5.ItwasfirstfoundtoinhibitM1muscarinicreceptorsstablytransfectedinCHOcellsatverylowconcentrations(1-30nM)6 andactsasanon-competitiveantagonistbybindingtoanallostericsite6.
MuscarinicToxin7bindingstudiesusingaM1andM3chimerademonstratedthatthehighaffinityofMuscarinicToxin7towardsM1receptorisduetoonlythreeresidueslocatedinthe2nd and3rd extracellularloopsofthereceptor7.
MuscarinicToxin7 (#STM-200) isahighlypure,synthetic,andbiologicallyactivepeptidetoxin.



