2017
Allosteric modulation of α4β2* nicotinic acetylcholine receptors: Desformylflustrabromine potentiates antiallodynic response of nicotine in a mouse model of neuropathic pain
Bagdas D, Ergun D, Jackson A, Toma W, Schulte M, Damaj M. Allosteric modulation of α4β2* nicotinic acetylcholine receptors: Desformylflustrabromine potentiates antiallodynic response of nicotine in a mouse model of neuropathic pain. European Journal Of Pain 2017, 22: 84-93. PMID: 28809075, PMCID: PMC9829446, DOI: 10.1002/ejp.1092.Peer-Reviewed Original ResearchConceptsPositive allosteric modulatorsChronic neuropathic painNeuropathic painΑ4β2 nAChRsNicotinic acetylcholine receptorsAllosteric modulationAcetylcholine receptorsAntagonist dihydro-β-erythroidineNeuronal nicotinic acetylcholine receptorsChronic constriction injuryEndogenous cholinergic toneNicotine-evoked responsesAnimal pain modelsNicotine-induced antinociceptionDihydro-β-erythroidineMediation of painAlternative treatment strategiesBehavior doseConstriction injuryAntiallodynic effectPain modelPain modulationCholinergic tonePain behaviorAntinociceptive properties
2015
In Vitro and in Vivo Neuronal Nicotinic Receptor Properties of (+)- and (−)-Pyrido[3,4]homotropane [(+)- and (−)-PHT]: (+)-PHT Is a Potent and Selective Full Agonist at α6β2 Containing Neuronal Nicotinic Acetylcholine Receptors
Carroll FI, Navarro H, Mascarella SW, Castro AH, Luetje CW, Wageman CR, Marks MJ, Jackson A, Damaj MI. In Vitro and in Vivo Neuronal Nicotinic Receptor Properties of (+)- and (−)-Pyrido[3,4]homotropane [(+)- and (−)-PHT]: (+)-PHT Is a Potent and Selective Full Agonist at α6β2 Containing Neuronal Nicotinic Acetylcholine Receptors. ACS Chemical Neuroscience 2015, 6: 920-926. PMID: 25891987, PMCID: PMC5589077, DOI: 10.1021/acschemneuro.5b00077.Peer-Reviewed Original ResearchMeSH KeywordsAlpha7 Nicotinic Acetylcholine ReceptorAnimalsConditioning, PsychologicalCorpus StriatumDopamineDose-Response Relationship, DrugMaleMice, Inbred ICRMolecular StructureNeuronsNicotinic AgonistsNicotinic AntagonistsPyridinesRatsReceptors, NicotinicSpatial BehaviorSynaptosomesTropanesXenopus laevisConceptsNicotinic antagonistsNeuronal nicotinic acetylcholine receptorsLow efficacy partial agonistSelective full agonistHot plate testNicotinic acetylcholine receptorsPlace preference studiesNicotine rewardAntinociceptive activityΑ3β4 nAChRsΑ7 nAChRsElectrophysiological studiesΑ4β2 nAChRsAcetylcholine receptorsAgonist activityPartial agonistFull agonistNAChRsFull agonismPartial agonismAntagonistΑ4β2MiceReceptor propertiesHigh potency