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- Kem,W.R. etal. (1997) J.Pharmacol.Exp.Therap. 283, 979.
- Weltzin,M.M. etal. (2010) J.Pharmacol. 334, 917.
- deFiebre,C.M. etal. (1995) Mol.Pharmacol. 47, 164.
AlomoneLabsDMAB-anabaseinedihydrochlorideinhibitsα7nicotinicacetylcholinereceptorsheterologouslyexpressedin Xenopus oocytes.A.Currenttracesofα7nicotinicacetylcholinereceptoractivityat-60mVholdingpotential.Currentswereelicitedbyapplicationof100µMacetylcholineevery50seconds.Inhibitionoftheseinducedcurrentswasachieveduponperfusionof1or10µM DMAB-anabaseinedihydrochloride (#D-110)(indicatedbyhorizontalbars).B.Superimposedcurrentresponsestotheapplicationofeither100µMacetylcholine(Ach)or100µMDMAB-anabaseinedihydrochloride(Ana),demonstratingthepartialagonisteffectonα7channels.
- 1.Kombo,D.C. etal. (2011) Eur.J.Med.Chem. 46,5625.
- 2.Papke,R.L. etal. (1994) GiacobiniE,BeckerR(eds)Alzheimerdisease: therapeuticstrategies,206.
- 3.deFiebre,C.M. etal. (1995) Mol.Pharmacol. 47, 164.
- 4.Kem,W.R. etal. (1997) J.Pharmacol.Exp.Therap. 283, 979.
- 5.Stevens,K.E. etal. (1998) Psychopharmacology 136, 320.
- 6.Weltzin,M.M. etal. (2010) J.Pharmacol. 334, 917.
nAChRsaremembersoftheCys-loopligand-gatedionchannelsuperfamily,locatedbothintheperipheralandcentralnervoussystems(PNSandCNS,respectively).Thesereceptors,existingasbothhomopentamericandheteropentamerictransmembraneionchannels,arevalidatedtherapeutictargetsforvariousCNSpathologies1.
DMAB-anabaseine(DMAB),ananabaseineanalog,isaselectivelypartialagonistatα7receptorswhicharepredominantlyfoundintheCNS2,3.Incontrast,DMABisanantagonistatα3β4,α4β2andothernicotinicreceptors4,5andblockstheα4β2currentwithIC50 ~5µM6.
DMAB-anabaseinedihydrochloride(#D-110) isahighlypure,synthetic,andbiologicallyactivecompound.



