2019
The α7 nicotinic receptor silent agonist R-47 prevents and reverses paclitaxel-induced peripheral neuropathy in mice without tolerance or altering nicotine reward and withdrawal
Toma W, Kyte SL, Bagdas D, Jackson A, Meade JA, Rahman F, Chen ZJ, Del Fabbro E, Cantwell L, Kulkarni A, Thakur GA, Papke RL, Bigbee JW, Gewirtz DA, Damaj MI. The α7 nicotinic receptor silent agonist R-47 prevents and reverses paclitaxel-induced peripheral neuropathy in mice without tolerance or altering nicotine reward and withdrawal. Experimental Neurology 2019, 320: 113010. PMID: 31299179, PMCID: PMC6708482, DOI: 10.1016/j.expneurol.2019.113010.Peer-Reviewed Original ResearchConceptsChemotherapy-induced peripheral neuropathyPeripheral neuropathyNicotine rewardPaclitaxel treatmentRewarding effectsTreatment of CIPNPaclitaxel-induced mechanical hypersensitivityTumor-bearing NSG micePaclitaxel-induced peripheral neuropathyNon-small cell lung cancer cell linesCell lung cancer cell linesA549 non-small cell lung cancer cell lineMecamylamine-precipitated withdrawalAntitumor activityIntraepidermal nerve fibersLung cancer cell linesLung tumor growthNSCLC cell viabilityTumor-bearing miceIntrinsic rewarding effectsPlace preference testCancer cell linesConditioned place preference testMechanical hypersensitivityAgonist R
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