2021
(E)-3-furan-2-yl-N-phenylacrylamide (PAM-4) decreases nociception and emotional manifestations of neuropathic pain in mice by α7 nicotinic acetylcholine receptor potentiation
Bagdas D, Sevdar G, Gul Z, Younis R, Cavun S, Tae HS, Ortells MO, Arias HR, Gurun MS. (E)-3-furan-2-yl-N-phenylacrylamide (PAM-4) decreases nociception and emotional manifestations of neuropathic pain in mice by α7 nicotinic acetylcholine receptor potentiation. Neurological Research 2021, 43: 1056-1068. PMID: 34281483, DOI: 10.1080/01616412.2021.1949684.Peer-Reviewed Original ResearchConceptsPositive allosteric modulationΑ7 nAChRsNeuropathic painΑ7-selective antagonist methyllycaconitineΑ7 nicotinic acetylcholine receptorChronic constriction injuryPaw licking behaviorNeuropathic pain modelAcute systemic administrationChronic painful conditionsAntidepressant-like activityAnti-nociceptive activityDepression-like behaviorAnxiogenic-like effectsNicotinic acetylcholine receptorsAffective behaviorHuman α7 nAChRConstriction injuryMechanical allodyniaFormalin testPain modelAntagonist methyllycaconitineChronic painPainful conditionsRat α7 nAChR
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