2018
The antinociceptive and anti-inflammatory properties of the α7 nAChR weak partial agonist p-CF3 N,N-diethyl-N’-phenylpiperazine
Quadri M, Bagdas D, Toma W, Stokes C, Horenstein N, Damaj M, Papke R. The antinociceptive and anti-inflammatory properties of the α7 nAChR weak partial agonist p-CF3 N,N-diethyl-N’-phenylpiperazine. Journal Of Pharmacology And Experimental Therapeutics 2018, 367: jpet.118.249904. PMID: 30111636, PMCID: PMC7593094, DOI: 10.1124/jpet.118.249904.Peer-Reviewed Original ResearchConceptsAntinociceptive activitySelective antagonist methyllycaconitineAnti-inflammatory therapyAnti-inflammatory componentsAnti-inflammatory propertiesPositive allosteric modulatorsNon-neuronal cellsNicotinic acetylcholine receptorsVivo antinociceptive activityAntiedema effectInflammatory painAntagonist methyllycaconitineChronic painInflammatory diseasesHeteromeric nAChRsReceptor subtypesElectrophysiological profileNoncompetitive antagonistAcetylcholine receptorsAgonist activityPartial agonistAllosteric modulatorsSuch drugsPromising drug targetSilent agonist
2014
The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor
Papke R, Bagdas D, Kulkarni A, Gould T, AlSharari S, Thakur G, Damaj M. The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor. Neuropharmacology 2014, 91: 34-42. PMID: 25497451, PMCID: PMC4312719, DOI: 10.1016/j.neuropharm.2014.12.002.Peer-Reviewed Original ResearchConceptsPositive allosteric modulatorsChronic painAntinociceptive activityΑ7 nicotinic acetylcholine receptorAnalgesic-like propertiesPain-induced aversionNerve injury modelAcute thermal painNon-neuronal cellsNicotinic acetylcholine receptorsImportant affective componentIon channelsNeuropathic painPain modelNociceptive behaviorInflammatory diseasesInjury modelNS6740Α7 nAChRsΑ7 receptorsThermal painPainAcetylcholine receptorsChannel activatorNeurological disorders