2019
Chapter 33 Targeting Nicotinic Acetylcholine Receptors for the Treatment of Pain
Bagdas D, Kyte S, Toma W, Gurun M, Damaj M. Chapter 33 Targeting Nicotinic Acetylcholine Receptors for the Treatment of Pain. 2019, 259-266. DOI: 10.1016/b978-0-12-813035-3.00033-2.Peer-Reviewed Original ResearchNicotinic acetylcholine receptorsAcetylcholine receptorsNAChR ligandsTreatment of painRecent animal studiesNarrow therapeutic windowPeripheral nervous systemPositive allosteric modulatorsAnalgesic efficacyPain managementChronic painNeuropathic conditionsImmune cellsNovel analgesicsTherapeutic windowAnimal modelsAnimal studiesHuman studiesNervous systemNicotinic agentsAllosteric modulatorsTherapeutic potentialPainPromising agentSilent agonist
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 agonistCurcumin acts as a positive allosteric modulator of α7-nicotinic acetylcholine receptors and reverses nociception in mouse models of inflammatory pain
El Nebrisi E, Bagdas D, Toma W, Al Samri H, Brodzik A, Alkhlaif Y, Yang K, Howarth F, Damaj I, Oz M. Curcumin acts as a positive allosteric modulator of α7-nicotinic acetylcholine receptors and reverses nociception in mouse models of inflammatory pain. Journal Of Pharmacology And Experimental Therapeutics 2018, 365: jpet.117.245068. PMID: 29339457, PMCID: PMC7947331, DOI: 10.1124/jpet.117.245068.Peer-Reviewed Original ResearchConceptsEffect of curcuminPositive allosteric modulatorsMouse modelVisceral painAntinociceptive effectNACh receptorsAcetylcholine receptorsAllosteric modulatorsΑ7 nicotinic acetylcholine receptorVisceral pain modelHuman nicotinic acetylcholine receptorNicotinic acetylcholine receptorsInflammatory painPain modelNociceptive behaviorReceptor agonistSignificant potentiationDependent ClLocomotor activityACh concentrationPainNociceptionReceptorsTonicG proteins
2017
Reversal of Nicotine Withdrawal Signs Through Positive Allosteric Modulation of α4β2 Nicotinic Acetylcholine Receptors in Male Mice
Hamouda AK, Jackson A, Bagdas D, Damaj M. Reversal of Nicotine Withdrawal Signs Through Positive Allosteric Modulation of α4β2 Nicotinic Acetylcholine Receptors in Male Mice. Nicotine & Tobacco Research 2017, 20: 903-907. PMID: 29059422, PMCID: PMC5991208, DOI: 10.1093/ntr/ntx183.Peer-Reviewed Original ResearchConceptsNicotine withdrawal symptomsSpontaneous nicotine withdrawalNicotine withdrawal signsNicotine withdrawalWithdrawal symptomsPositive allosteric modulatorsCessation aidWithdrawal signsMale miceMouse modelAllosteric modulatorsNicotinic acetylcholine receptor agonistNAChR-positive allosteric modulatorsAcetylcholine receptor agonistDose-dependent reversalICR male miceΑ4β2 nicotinic acetylcholine receptorsPositive allosteric modulationAnxiety-like behaviorNicotinic acetylcholine receptorsPotential clinical useAcute injectionRelapse rateTobacco smokingDay infusion
2015
The Antinociceptive and Antiinflammatory Properties of 3-furan-2-yl-N-p-tolyl-acrylamide, a Positive Allosteric Modulator of &agr;7 Nicotinic Acetylcholine Receptors in Mice
Bagdas D, Targowska-Duda K, López J, Perez E, Arias H, Damaj M. The Antinociceptive and Antiinflammatory Properties of 3-furan-2-yl-N-p-tolyl-acrylamide, a Positive Allosteric Modulator of &agr;7 Nicotinic Acetylcholine Receptors in Mice. Anesthesia & Analgesia 2015, 121: 1369-1377. PMID: 26280585, PMCID: PMC4847442, DOI: 10.1213/ane.0000000000000902.Peer-Reviewed Original ResearchConceptsPositive allosteric modulatorsType II positive allosteric modulatorsNeuropathic pain modelInflammatory painNicotinic acetylcholine receptorsNeuropathic painPain modelCarrageenan testAntiinflammatory propertiesChronic constriction injury-induced neuropathic painAcetylcholine receptorsInjury-induced neuropathic painAllosteric modulatorsΑ7 nicotinic acetylcholine receptorSelective α7 agonistPlace aversion (CPA) testExperience of painEfficacy of agonistsEndogenous neurotransmissionMechanical allodyniaThermal hyperalgesiaTime-dependent mannerAntinociceptive effectComplete Freund'sPaw edema
2014
Nicotinic Receptors as Targets for Novel Analgesics and Anti-inflammatory Drugs
Damaj M, Freitas K, Bagdas D, Flood P. Nicotinic Receptors as Targets for Novel Analgesics and Anti-inflammatory Drugs. The Receptors 2014, 26: 239-254. DOI: 10.1007/978-1-4939-1167-7_12.Peer-Reviewed Original ResearchPositive allosteric modulatorsNicotinic receptorsNovel analgesicsTherapeutic windowChronic inflammatory pain conditionsAllosteric modulatorsInflammatory pain conditionsRecent animal studiesNarrow therapeutic windowPeripheral nervous systemAnti-inflammatory drugsAnalgesic efficacyPain controlPain conditionsΑ7 agonistsImmune cellsSelective α4β2Animal modelsHuman studiesAnimal studiesNervous systemNicotinic agentsTherapeutic potentialAgonistsAnalgesics