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Cocaine potently blocks neuronal α3β4 nicotinic acetylcholine receptors in SH-SY5Y cells.

Ma ZG, Jiang N, Huang YB, Ma XK, Brek Eaton J, Gao M, Chang YC, Lukas RJ, Whiteaker P, Neisewander J, Wu J.

Acta Pharmacol Sin. 2019 Aug 9. doi: 10.1038/s41401-019-0276-y. [Epub ahead of print]


Distinctive single-channel properties of α4β2-nicotinic acetylcholine receptor isoforms.

Weltzin MM, George AA, Lukas RJ, Whiteaker P.

PLoS One. 2019 Mar 7;14(3):e0213143. doi: 10.1371/journal.pone.0213143. eCollection 2019.


Alpha6-containing nicotinic acetylcholine receptor is a highly sensitive target of alcohol.

Gao F, Chen D, Ma X, Sudweeks S, Yorgason JT, Gao M, Turner D, Eaton JB, McIntosh JM, Lukas RJ, Whiteaker P, Chang Y, Steffensen SC, Wu J.

Neuropharmacology. 2019 May 1;149:45-54. doi: 10.1016/j.neuropharm.2019.01.021. Epub 2019 Jan 30.


Roles of Nicotine in the Development of Intracranial Aneurysm Rupture.

Kamio Y, Miyamoto T, Kimura T, Mitsui K, Furukawa H, Zhang D, Yokosuka K, Korai M, Kudo D, Lukas RJ, Lawton MT, Hashimoto T.

Stroke. 2018 Oct;49(10):2445-2452. doi: 10.1161/STROKEAHA.118.021706.


α1-FANGs: Protein Ligands Selective for the α-Bungarotoxin Site of the α1-Nicotinic Acetylcholine Receptor.

Nichols AL, Noridomi K, Hughes CR, Jalali-Yazdi F, Eaton JB, Lai LH, Advani G, Lukas RJ, Lester HA, Chen L, Roberts RW.

ACS Chem Biol. 2018 Sep 21;13(9):2568-2576. doi: 10.1021/acschembio.8b00513. Epub 2018 Aug 13.


Pharmacological and functional comparisons of α6/α3β2β3-nAChRs and α4β2-nAChRs heterologously expressed in the human epithelial SH-EP1 cell line.

Chen DJ, Gao FF, Ma XK, Shi GG, Huang YB, Su QX, Sudweeks S, Gao M, Dharshaun T, Eaton JB, Chang YC, Mcintosh JM, Lukas RJ, Whiteaker P, Steffensen SC, Wu J.

Acta Pharmacol Sin. 2018 Oct;39(10):1571-1581. doi: 10.1038/aps.2017.209. Epub 2018 May 24.


Distinctive Roles for α7*- and α9*-Nicotinic Acetylcholine Receptors in Inflammatory and Autoimmune Responses in the Murine Experimental Autoimmune Encephalomyelitis Model of Multiple Sclerosis.

Liu Q, Whiteaker P, Morley BJ, Shi FD, Lukas RJ.

Front Cell Neurosci. 2017 Sep 22;11:287. doi: 10.3389/fncel.2017.00287. eCollection 2017.


Isoform-specific mechanisms of α3β4*-nicotinic acetylcholine receptor modulation by the prototoxin lynx1.

George AA, Bloy A, Miwa JM, Lindstrom JM, Lukas RJ, Whiteaker P.

FASEB J. 2017 Apr;31(4):1398-1420. doi: 10.1096/fj.201600733R. Epub 2017 Jan 18.


Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists.

Zhang HK, Eaton JB, Fedolak A, Gunosewoyo H, Onajole OK, Brunner D, Lukas RJ, Yu LF, Kozikowski AP.

Eur J Med Chem. 2016 Nov 29;124:689-697. doi: 10.1016/j.ejmech.2016.09.016. Epub 2016 Sep 9.


Emamectin is a non-selective allosteric activator of nicotinic acetylcholine receptors and GABAA/C receptors.

Xu X, Sepich C, Lukas RJ, Zhu G, Chang Y.

Biochem Biophys Res Commun. 2016 May 13;473(4):795-800. doi: 10.1016/j.bbrc.2016.03.097. Epub 2016 Apr 2.


Synthesis and Behavioral Studies of Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part III.

Onajole OK, Vallerini GP, Eaton JB, Lukas RJ, Brunner D, Caldarone BJ, Kozikowski AP.

ACS Chem Neurosci. 2016 Jun 15;7(6):811-22. doi: 10.1021/acschemneuro.6b00050. Epub 2016 Apr 21.


Differential α4(+)/(-)β2 Agonist-binding Site Contributions to α4β2 Nicotinic Acetylcholine Receptor Function within and between Isoforms.

Lucero LM, Weltzin MM, Eaton JB, Cooper JF, Lindstrom JM, Lukas RJ, Whiteaker P.

J Biol Chem. 2016 Jan 29;291(5):2444-59. doi: 10.1074/jbc.M115.684373. Epub 2015 Dec 7.


Distinctive effects of nicotinic receptor intracellular-loop mutations associated with nocturnal frontal lobe epilepsy.

Weltzin MM, Lindstrom JM, Lukas RJ, Whiteaker P.

Neuropharmacology. 2016 Mar;102:158-73. doi: 10.1016/j.neuropharm.2015.11.004. Epub 2015 Nov 10.


Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor.

Zhang Q, Du Y, Zhang J, Xu X, Xue F, Guo C, Huang Y, Lukas RJ, Chang Y.

PLoS One. 2015 Sep 4;10(9):e0137588. doi: 10.1371/journal.pone.0137588. eCollection 2015.


Resistance to Inhibitors of Cholinesterase 3 (Ric-3) Expression Promotes Selective Protein Associations with the Human α7-Nicotinic Acetylcholine Receptor Interactome.

Mulcahy MJ, Blattman SB, Barrantes FJ, Lukas RJ, Hawrot E.

PLoS One. 2015 Aug 10;10(8):e0134409. doi: 10.1371/journal.pone.0134409. eCollection 2015.


Roles of nicotinic acetylcholine receptor β subunit cytoplasmic loops in acute desensitization and single-channel features.

Liu Q, Kuo YP, Shen J, Lukas RJ, Wu J.

Neuroscience. 2015 Mar 19;289:315-23. doi: 10.1016/j.neuroscience.2014.12.016. Epub 2014 Dec 20.


The potent and selective α4β2*/α6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-((S)Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile.

Yu LF, Brek Eaton J, Zhang HK, Sabath E, Hanania T, Li GN, van Breemen RB, Whiteaker P, Liu Q, Wu J, Chang YC, Lukas RJ, Brunner D, Kozikowski AP.

Pharmacol Res Perspect. 2014 Apr;2(2):e00026. doi: 10.1002/prp2.26. Epub 2014 Mar 12.


Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands.

Onajole OK, Eaton JB, Lukas RJ, Brunner D, Thiede L, Caldarone BJ, Kozikowski AP.

ACS Med Chem Lett. 2014 Sep 29;5(11):1196-201. doi: 10.1021/ml500129k. eCollection 2014 Nov 13.


The novel α7β2-nicotinic acetylcholine receptor subtype is expressed in mouse and human basal forebrain: biochemical and pharmacological characterization.

Moretti M, Zoli M, George AA, Lukas RJ, Pistillo F, Maskos U, Whiteaker P, Gotti C.

Mol Pharmacol. 2014 Sep;86(3):306-17. doi: 10.1124/mol.114.093377. Epub 2014 Jul 7.


Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.

Yu LF, Zhang HK, Caldarone BJ, Eaton JB, Lukas RJ, Kozikowski AP.

J Med Chem. 2014 Oct 23;57(20):8204-23. doi: 10.1021/jm401937a. Epub 2014 Jul 2. Review.


Bupropion and bupropion analogs as treatments for CNS disorders.

Carroll FI, Blough BE, Mascarella SW, Navarro HA, Lukas RJ, Damaj MI.

Adv Pharmacol. 2014;69:177-216. doi: 10.1016/B978-0-12-420118-7.00005-6. Review.


A signal peptide missense mutation associated with nicotine dependence alters α2*-nicotinic acetylcholine receptor function.

Dash B, Lukas RJ, Li MD.

Neuropharmacology. 2014 Apr;79:715-25. doi: 10.1016/j.neuropharm.2014.01.021. Epub 2014 Jan 24.


The unique α4+/-α4 agonist binding site in (α4)3(β2)2 subtype nicotinic acetylcholine receptors permits differential agonist desensitization pharmacology versus the (α4)2(β2)3 subtype.

Eaton JB, Lucero LM, Stratton H, Chang Y, Cooper JF, Lindstrom JM, Lukas RJ, Whiteaker P.

J Pharmacol Exp Ther. 2014 Jan;348(1):46-58. doi: 10.1124/jpet.113.208389. Epub 2013 Nov 4.


Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II.

Zhang HK, Yu LF, Eaton JB, Whiteaker P, Onajole OK, Hanania T, Brunner D, Lukas RJ, Kozikowski AP.

J Med Chem. 2013 Jul 11;56(13):5495-504. doi: 10.1021/jm400510u. Epub 2013 Jun 26.


A novel nicotinic mechanism underlies β-amyloid-induced neuronal hyperexcitation.

Liu Q, Xie X, Lukas RJ, St John PA, Wu J.

J Neurosci. 2013 Apr 24;33(17):7253-63. doi: 10.1523/JNEUROSCI.3235-12.2013.


Differential modulation of EAE by α9*- and β2*-nicotinic acetylcholine receptors.

Simard AR, Gan Y, St-Pierre S, Kousari A, Patel V, Whiteaker P, Morley BJ, Lukas RJ, Shi FD.

Immunol Cell Biol. 2013 Mar;91(3):195-200. doi: 10.1038/icb.2013.1. Epub 2013 Feb 12.


Nicotine-morphine interactions at α4β2, α7 and α3(⁎) nicotinic acetylcholine receptors.

Talka R, Salminen O, Whiteaker P, Lukas RJ, Tuominen RK.

Eur J Pharmacol. 2013 Feb 15;701(1-3):57-64. doi: 10.1016/j.ejphar.2013.01.005. Epub 2013 Jan 20.


Discovery of highly potent and selective α4β2-nicotinic acetylcholine receptor (nAChR) partial agonists containing an isoxazolylpyridine ether scaffold that demonstrate antidepressant-like activity. Part II.

Yu LF, Eaton JB, Fedolak A, Zhang HK, Hanania T, Brunner D, Lukas RJ, Kozikowski AP.

J Med Chem. 2012 Nov 26;55(22):9998-10009. doi: 10.1021/jm301177j. Epub 2012 Nov 2.


Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.

Breining SR, Melvin M, Bhatti BS, Byrd GD, Kiser MN, Hepler CD, Hooker DN, Zhang J, Reynolds LA, Benson LR, Fedorov NB, Sidach SS, Mitchener JP, Lucero LM, Lukas RJ, Whiteaker P, Yohannes D.

J Med Chem. 2012 Nov 26;55(22):9929-45. doi: 10.1021/jm3011299. Epub 2012 Oct 17.


Impact of prefrontal cortex in nicotine-induced excitation of ventral tegmental area dopamine neurons in anesthetized rats.

Zhang D, Gao M, Xu D, Shi WX, Gutkin BS, Steffensen SC, Lukas RJ, Wu J.

J Neurosci. 2012 Sep 5;32(36):12366-75.


Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands to α4β2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands.

Zhang HK, Eaton JB, Yu LF, Nys M, Mazzolari A, van Elk R, Smit AB, Alexandrov V, Hanania T, Sabath E, Fedolak A, Brunner D, Lukas RJ, Vistoli G, Ulens C, Kozikowski AP.

J Med Chem. 2012 Sep 27;55(18):8028-37. Epub 2012 Sep 7.


Function of human α3β4α5 nicotinic acetylcholine receptors is reduced by the α5(D398N) variant.

George AA, Lucero LM, Damaj MI, Lukas RJ, Chen X, Whiteaker P.

J Biol Chem. 2012 Jul 20;287(30):25151-62. doi: 10.1074/jbc.M112.379339. Epub 2012 Jun 4.


Modulation of gain-of-function α6*-nicotinic acetylcholine receptor by β3 subunits.

Dash B, Lukas RJ.

J Biol Chem. 2012 Apr 20;287(17):14259-69. doi: 10.1074/jbc.M111.322610. Epub 2012 Feb 7.


Modulation of recombinant, α2*, α3* or α4*-nicotinic acetylcholine receptor (nAChR) function by nAChR β3 subunits.

Dash B, Bhakta M, Chang Y, Lukas RJ.

J Neurochem. 2012 May;121(3):349-61. doi: 10.1111/j.1471-4159.2012.07685.x. Epub 2012 Mar 14.


Chemistry and behavioral studies identify chiral cyclopropanes as selective α4β2-nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile.

Zhang H, Tückmantel W, Eaton JB, Yuen PW, Yu LF, Bajjuri KM, Fedolak A, Wang D, Ghavami A, Caldarone B, Paterson NE, Lowe DA, Brunner D, Lukas RJ, Kozikowski AP.

J Med Chem. 2012 Jan 26;55(2):717-24. doi: 10.1021/jm201157c. Epub 2012 Jan 10.


Identification of novel α4β2-nicotinic acetylcholine receptor (nAChR) agonists based on an isoxazole ether scaffold that demonstrate antidepressant-like activity.

Yu LF, Tückmantel W, Eaton JB, Caldarone B, Fedolak A, Hanania T, Brunner D, Lukas RJ, Kozikowski AP.

J Med Chem. 2012 Jan 26;55(2):812-23. doi: 10.1021/jm201301h. Epub 2012 Jan 4.


α7β2 nicotinic acetylcholine receptors assemble, function, and are activated primarily via their α7-α7 interfaces.

Murray TA, Bertrand D, Papke RL, George AA, Pantoja R, Srinivasan R, Liu Q, Wu J, Whiteaker P, Lester HA, Lukas RJ.

Mol Pharmacol. 2012 Feb;81(2):175-88. doi: 10.1124/mol.111.074088. Epub 2011 Oct 28. Erratum in: Mol Pharmacol. 2016 Sep;90(3):410.


Discovery of isoxazole analogues of sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression.

Liu J, Yu LF, Eaton JB, Caldarone B, Cavino K, Ruiz C, Terry M, Fedolak A, Wang D, Ghavami A, Lowe DA, Brunner D, Lukas RJ, Kozikowski AP.

J Med Chem. 2011 Oct 27;54(20):7280-8. doi: 10.1021/jm200855b. Epub 2011 Sep 30.


Reporter mutation studies show that nicotinic acetylcholine receptor (nAChR) α5 Subunits and/or variants modulate function of α6*-nAChR.

Dash B, Chang Y, Lukas RJ.

J Biol Chem. 2011 Nov 4;286(44):37905-18. doi: 10.1074/jbc.M111.264044. Epub 2011 Aug 26.


Naturally-expressed nicotinic acetylcholine receptor subtypes.

Wu J, Lukas RJ.

Biochem Pharmacol. 2011 Oct 15;82(8):800-7. doi: 10.1016/j.bcp.2011.07.067. Epub 2011 Jul 20. Review.


Desensitization of alpha7 nicotinic receptor is governed by coupling strength relative to gate tightness.

Zhang J, Xue F, Whiteaker P, Li C, Wu W, Shen B, Huang Y, Lukas RJ, Chang Y.

J Biol Chem. 2011 Jul 15;286(28):25331-40. doi: 10.1074/jbc.M111.221754. Epub 2011 May 24.


Functional nicotinic acetylcholine receptors containing α6 subunits are on GABAergic neuronal boutons adherent to ventral tegmental area dopamine neurons.

Yang K, Buhlman L, Khan GM, Nichols RA, Jin G, McIntosh JM, Whiteaker P, Lukas RJ, Wu J.

J Neurosci. 2011 Feb 16;31(7):2537-48. doi: 10.1523/JNEUROSCI.3003-10.2011.


Synthesis of 2-(substituted phenyl)-3,5,5-trimethylmorpholine analogues and their effects on monoamine uptake, nicotinic acetylcholine receptor function, and behavioral effects of nicotine.

Carroll FI, Muresan AZ, Blough BE, Navarro HA, Mascarella SW, Eaton JB, Huang X, Damaj MI, Lukas RJ.

J Med Chem. 2011 Mar 10;54(5):1441-8. doi: 10.1021/jm1014555. Epub 2011 Feb 14.


Intravenous hedgehog agonist induces proliferation of neural and oligodendrocyte precursors in rodent spinal cord injury.

Bambakidis NC, Wang X, Lukas RJ, Spetzler RF, Sonntag VK, Preul MC.

Neurosurgery. 2010 Dec;67(6):1709-15; discussion 1715. doi: 10.1227/NEU.0b013e3181f9b0a5.


Nicotinic acetylcholine receptor efficacy and pharmacological properties of 3-(substituted phenyl)-2β-substituted tropanes.

Carroll FI, Blough BE, Mascarella SW, Navarro HA, Eaton JB, Lukas RJ, Damaj MI.

J Med Chem. 2010 Dec 9;53(23):8345-53. doi: 10.1021/jm100994w. Epub 2010 Nov 8.


Mechanisms involved in systemic nicotine-induced glutamatergic synaptic plasticity on dopamine neurons in the ventral tegmental area.

Gao M, Jin Y, Yang K, Zhang D, Lukas RJ, Wu J.

J Neurosci. 2010 Oct 13;30(41):13814-25. doi: 10.1523/JNEUROSCI.1943-10.2010.


Attenuation of CNS inflammatory responses by nicotine involves α7 and non-α7 nicotinic receptors.

Hao J, Simard AR, Turner GH, Wu J, Whiteaker P, Lukas RJ, Shi FD.

Exp Neurol. 2011 Jan;227(1):110-9. doi: 10.1016/j.expneurol.2010.09.020. Epub 2010 Oct 13.

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