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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.
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(-)-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.