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- Albuquerque,E.X. etal. (2009) Physiol.Rev. 89,73.
- Luetje,C.W.andPatrick,J. (1991) J.Neurosci. 11,837.
AlomoneLabs(-)-Cytisineactivatesα2/β4nicotinicacetylcholinereceptorchannelsheterologouslyexpressedin Xenopus oocytes.Currenttracesofα2/β4nicotinicacetylcholinereceptorchannelsactivityat-60mVholdingpotential.Thebarsabovethetracerepresentperiodswhere (-)-Cytisine (#C-130)oracetylcholinewereappliedattheindicatedconcentration.
- 1.Banko,P.C. etal. (2002) J.Chem.Ecol. 28, 1393.
- 2.Albuquerque,E.X. etal. (2009) Physiol.Rev. 89, 73.
- 3.Luetje,C.W.andPatrick,J. (1991) J.Neurosci. 11, 837.
- 4.Chavez-Noriega,L.E. etal. (1997) J.Pharmacol.Exp.Ther. 280, 346.
- 5.Papke,R.L.andHeinemann,S.F. (1994) Mol.Pharmacol. 45, 142.
- 6.Mineur,Y.S. etal. (2007) Neuropharmacology 52, 1256.
- 7.Reavill,C. etal. (1990) Neuropharmacology 29, 619.
(-)-Cytisineisanalkaloid,whichoccursnaturallyinseveraltypesofplantsaswellasinanimalsfeedingonthem(seeexampleinreference1).(-)-CytisineisapotentandselectiveagonistofneuronalnAChR2.Itactsasapartialagonistofβ2-containingnAChR3.
EC50sdifferfordifferentsubunit-composedchannels;forrecombinanthumanchannelsexpressedinXenopusoocytesthefollowingEC50valueswerereported:25µM,39µM,67µM,72µM,2.6µM0.9µMand71µMforα2/β2,α2/β4,α3/β2,α3/β4,α4/β2,α4/β4andα7respectively4.
However,inβ2-containingchannels,theresponsetoacetylcholine(ACh)islargelyreducedwhenappliedincombinationwith(-)-Cytisine5.Therefore,whenappliedinvivoitexertsacompoundeffectofbothactivatingcertainnAchRsandinhibitingtheeffectofAChonothers.Forexample,(-)-Cytisinewasfoundtohaveantidepressant-likeeffectsinseveralanimalmodelsofantidepressantefficacy.ThiswasprobablyachievedbyinhibitingtheeffectofAChonα2/β4channelinthebasolateralamygdala6.
Inanotherstudy,theeffectsof(-)-Cytisinewerecomparedtonicotine.Ratsweretrainedtodiscriminatenicotinefromsalineanditwasconfirmedthat(-)-Cytisinehadanicotine-likediscriminativeeffect,butitwasmuchlesspotentthannicotineitself7.
(-)-Cytisine(#C-130) isahighlypure,synthetic,andbiologicallyactivecompound.
