2022
Pharmacological characterization of 5-iodo-A-85380, a β2-selective nicotinic receptor agonist, in mice
Akinola LS, Bagdas D, Alkhlaif Y, Jackson A, Gurdap CO, Rahimpour E, Carroll FI, Papke RL, Damaj MI. Pharmacological characterization of 5-iodo-A-85380, a β2-selective nicotinic receptor agonist, in mice. Journal Of Psychopharmacology 2022, 36: 1280-1293. PMID: 36321267, PMCID: PMC9817006, DOI: 10.1177/02698811221132214.Peer-Reviewed Original ResearchConceptsNicotinic receptor agonistsReceptor agonistNicotinic acetylcholine receptorsLow sensitivityPharmacological characterizationΑ4β2 receptorsNicotine dependenceNicotinic subunitsPlace preferenceΑ4β2 nAChRsAcetylcholine receptorsPartial agonistFull agonistAgonistsDifferential efficacyBehavioral effectsNeurodegenerative diseasesSubtypesPathological conditionsNAChRsPotential targetPotential roleHypothermiaReceptorsΑ6
2021
Potentiation of (α4)2(β2)3, but not (α4)3(β2)2, nicotinic acetylcholine receptors reduces nicotine self-administration and withdrawal symptoms
Hamouda AK, Bautista MR, Akinola LS, Alkhlaif Y, Jackson A, Carper M, Toma WB, Garai S, Chen YC, Thakur GA, Fowler CD, Damaj MI. Potentiation of (α4)2(β2)3, but not (α4)3(β2)2, nicotinic acetylcholine receptors reduces nicotine self-administration and withdrawal symptoms. Neuropharmacology 2021, 190: 108568. PMID: 33878302, PMCID: PMC8169606, DOI: 10.1016/j.neuropharm.2021.108568.Peer-Reviewed Original ResearchConceptsPositive allosteric modulatorsWithdrawal symptomsHypothermic effectMale miceAntinociceptive effectΑ4β2 nAChRsNicotine withdrawal-induced hyperalgesiaNAChR isoformsNicotine's antinociceptive effectsWithdrawal-induced hyperalgesiaNicotine withdrawal symptomsNicotine addiction treatmentAnxiety-like behaviorNicotinic acetylcholine receptorsDose-dependent mannerNociceptive responsesNicotine withdrawalNicotine intakeSomatic signsNicotine abstinencePharmacological effectsNicotine useAcetylcholine receptorsAffective symptomsPathophysiological processes
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