2013
Differential Modulation of Brain Nicotinic Acetylcholine Receptor Function by Cytisine, Varenicline, and Two Novel Bispidine Compounds: Emergent Properties of a Hybrid Molecule
Peng C, Stokes C, Mineur YS, Picciotto MR, Tian C, Eibl C, Tomassoli I, Guendisch D, Papke RL. Differential Modulation of Brain Nicotinic Acetylcholine Receptor Function by Cytisine, Varenicline, and Two Novel Bispidine Compounds: Emergent Properties of a Hybrid Molecule. Journal Of Pharmacology And Experimental Therapeutics 2013, 347: 424-437. PMID: 23959137, PMCID: PMC3807070, DOI: 10.1124/jpet.113.206904.Peer-Reviewed Original ResearchMeSH KeywordsAlkaloidsAnimalsAzocinesBehavior, AnimalBenzazepinesBrainBridged Bicyclo Compounds, HeterocyclicDose-Response Relationship, DrugDrug Partial AgonismHEK293 CellsHumansMaleMembrane PotentialsMiceMolecular StructureNicotinic AgonistsOocytesPatch-Clamp TechniquesQuinolizinesQuinoxalinesRatsRats, Sprague-DawleyReceptors, NicotinicTobacco Use DisorderVareniclineXenopus laevisConceptsPartial agonistLGN neuronsMouse tail suspension testLateral geniculate nucleus neuronsNicotinic acetylcholine receptor functionPartial agonist therapiesTail suspension testStratum radiatum interneuronsSmoking cessation drugNicotinic partial agonistAcetylcholine receptor functionHuman embryonic kidney 293 cellsSteady-state activationAgonist therapyRadiatum interneuronsEmbryonic kidney 293 cellsCessation drugsNucleus neuronsSuspension testΑ7 currentsNicotine addictionSide effectsVareniclineΑ4β2 nAChRsSR interneurons
2000
Nicotinic-agonist stimulated 86Rb+ efflux and [3H]epibatidine binding of mice differing in β2 genotype
Marks M, Stitzel J, Grady S, Picciotto M, Changeux J, Collins A. Nicotinic-agonist stimulated 86Rb+ efflux and [3H]epibatidine binding of mice differing in β2 genotype. Neuropharmacology 2000, 39: 2632-2645. PMID: 11044733, DOI: 10.1016/s0028-3908(00)00115-5.Peer-Reviewed Original ResearchConceptsBrain regionsNicotinic acetylcholine receptor functionBeta2 subunitBeta2-containing receptorsAcetylcholine receptor functionHigh-affinity siteBeta2 subunit expressionBinding of mouseCerebral cortexNicotinic responsesMicroM nicotineOlfactory bulbInferior colliculusNicotinic agonistsSubunit expressionReceptor functionLow affinityLow affinity sitesDHbetaEInhibitionMiceStimulationEffluxCytisineNull mutationPharmacological and null mutation approaches reveal nicotinic receptor diversity
Whiteaker P, Marks M, Grady S, Lu Y, Picciotto M, Changeux J, Collins A. Pharmacological and null mutation approaches reveal nicotinic receptor diversity. European Journal Of Pharmacology 2000, 393: 123-135. PMID: 10771005, DOI: 10.1016/s0014-2999(00)00052-2.Peer-Reviewed Reviews, Practice Guidelines, Standards, and Consensus StatementsConceptsNicotinic acetylcholine receptor functionNicotinic acetylcholine receptorsAcetylcholine receptor functionAcetylcholine receptorsNicotinic acetylcholine receptor bindingReceptor functionNative nicotinic acetylcholine receptorsNicotinic acetylcholine receptor subtypesWhole brain preparationAcetylcholine receptor bindingAcetylcholine receptor subtypesMouse brain membranesArray of assaysReceptor subtypesPharmacological comparisonComparative pharmacologyBrain nucleiBrain membranesEfflux techniqueReceptor bindingSubunit deletionReceptor diversityReceptorsAminobutyric acidSubtypes