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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]


PeIA-5466: A Novel Peptide Antagonist Containing Non-natural Amino Acids That Selectively Targets α3β2 Nicotinic Acetylcholine Receptors.

Hone AJ, Fisher F, Christensen S, Gajewiak J, Larkin D, Whiteaker P, McIntosh JM.

J Med Chem. 2019 Jul 11;62(13):6262-6275. doi: 10.1021/acs.jmedchem.9b00566. Epub 2019 Jun 27.


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.


Cocaine Directly Inhibits α6-Containing Nicotinic Acetylcholine Receptors in Human SH-EP1 Cells and Mouse VTA DA Neurons.

Chen D, Gao F, Ma X, Eaton JB, Huang Y, Gao M, Chang Y, Ma Z, Der-Ghazarian T, Neisewander J, Whiteaker P, Wu J, Su Q.

Front Pharmacol. 2019 Feb 14;10:72. doi: 10.3389/fphar.2019.00072. 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.


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.


Commentary: Nicotinic Acetylcholine Receptor α9 and α10 Subunits Are Expressed in the Brain of Mice.

Morley BJ, Whiteaker P, Elgoyhen AB.

Front Cell Neurosci. 2018 May 1;12:104. doi: 10.3389/fncel.2018.00104. eCollection 2018. No abstract available.


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.


Heteromeric α7β2 Nicotinic Acetylcholine Receptors in the Brain.

Wu J, Liu Q, Tang P, Mikkelsen JD, Shen J, Whiteaker P, Yakel JL.

Trends Pharmacol Sci. 2016 Jul;37(7):562-574. doi: 10.1016/ Epub 2016 May 11. Review.


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.


The prototoxin LYPD6B modulates heteromeric α3β4-containing nicotinic acetylcholine receptors, but not α7 homomers.

Ochoa V, George AA, Nishi R, Whiteaker P.

FASEB J. 2016 Mar;30(3):1109-19. doi: 10.1096/fj.15-274548. Epub 2015 Nov 19.


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.


α-Conotoxins Identify the α3β4* Subtype as the Predominant Nicotinic Acetylcholine Receptor Expressed in Human Adrenal Chromaffin Cells.

Hone AJ, McIntosh JM, Azam L, Lindstrom J, Lucero L, Whiteaker P, Passas J, Blázquez J, Albillos A.

Mol Pharmacol. 2015 Nov;88(5):881-93. doi: 10.1124/mol.115.100982. Epub 2015 Sep 1. Erratum in: Mol Pharmacol. 2016 Feb;89(2):322.


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.


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.


α6β2*-subtype nicotinic acetylcholine receptors are more sensitive than α4β2*-subtype receptors to regulation by chronic nicotine administration.

Marks MJ, Grady SR, Salminen O, Paley MA, Wageman CR, McIntosh JM, Whiteaker P.

J Neurochem. 2014 Jul;130(2):185-98. doi: 10.1111/jnc.12721. Epub 2014 Apr 19.


A novel α4/7-conotoxin LvIA from Conus lividus that selectively blocks α3β2 vs. α6/α3β2β3 nicotinic acetylcholine receptors.

Luo S, Zhangsun D, Schroeder CI, Zhu X, Hu Y, Wu Y, Weltzin MM, Eberhard S, Kaas Q, Craik DJ, McIntosh JM, Whiteaker P.

FASEB J. 2014 Apr;28(4):1842-53. doi: 10.1096/fj.13-244103. Epub 2014 Jan 7.


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.


Nicotinic receptor β2 determines NK cell-dependent metastasis in a murine model of metastatic lung cancer.

Hao J, Shi FD, Abdelwahab M, Shi SX, Simard A, Whiteaker P, Lukas R, Zhou Q.

PLoS One. 2013;8(2):e57495. doi: 10.1371/journal.pone.0057495. Epub 2013 Feb 28.


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.


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.


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.


A novel α-conotoxin MII-sensitive nicotinic acetylcholine receptor modulates [(3) H]-GABA release in the superficial layers of the mouse superior colliculus.

McClure-Begley TD, Wageman CR, Grady SR, Marks MJ, McIntosh JM, Collins AC, Whiteaker P.

J Neurochem. 2012 Jul;122(1):48-57. doi: 10.1111/j.1471-4159.2012.07759.x. Epub 2012 May 9.


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.


Progress and challenges in the study of α6-containing nicotinic acetylcholine receptors.

Letchworth SR, Whiteaker P.

Biochem Pharmacol. 2011 Oct 15;82(8):862-72. doi: 10.1016/j.bcp.2011.06.022. Epub 2011 Jun 28. 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.


Increased nicotinic acetylcholine receptor protein underlies chronic nicotine-induced up-regulation of nicotinic agonist binding sites in mouse brain.

Marks MJ, McClure-Begley TD, Whiteaker P, Salminen O, Brown RW, Cooper J, Collins AC, Lindstrom JM.

J Pharmacol Exp Ther. 2011 Apr;337(1):187-200. doi: 10.1124/jpet.110.178236. Epub 2011 Jan 12.


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.


A component of Premarin(®) enhances multiple cognitive functions and influences nicotinic receptor expression.

Talboom JS, Engler-Chiurazzi EB, Whiteaker P, Simard AR, Lukas R, Acosta JI, Prokai L, Bimonte-Nelson HA.

Horm Behav. 2010 Nov;58(5):917-28. doi: 10.1016/j.yhbeh.2010.09.002. Epub 2010 Sep 19.


Mechanism of Allosteric Modulation of the Cys-loop Receptors.

Chang Y, Huang Y, Whiteaker P.

Pharmaceuticals (Basel). 2010 Aug 12;3(8):2592-2609. Review.


Alexa Fluor 546-ArIB[V11L;V16A] is a potent ligand for selectively labeling alpha 7 nicotinic acetylcholine receptors.

Hone AJ, Whiteaker P, Mohn JL, Jacob MH, McIntosh JM.

J Neurochem. 2010 Aug;114(4):994-1006. doi: 10.1111/j.1471-4159.2010.06819.x. Epub 2010 May 18.


Structural differences determine the relative selectivity of nicotinic compounds for native alpha 4 beta 2*-, alpha 6 beta 2*-, alpha 3 beta 4*- and alpha 7-nicotine acetylcholine receptors.

Grady SR, Drenan RM, Breining SR, Yohannes D, Wageman CR, Fedorov NB, McKinney S, Whiteaker P, Bencherif M, Lester HA, Marks MJ.

Neuropharmacology. 2010 Jun;58(7):1054-66. doi: 10.1016/j.neuropharm.2010.01.013. Epub 2010 Jan 28.


Dopamine D2-receptor activation elicits akinesia, rigidity, catalepsy, and tremor in mice expressing hypersensitive {alpha}4 nicotinic receptors via a cholinergic-dependent mechanism.

Zhao-Shea R, Cohen BN, Just H, McClure-Begley T, Whiteaker P, Grady SR, Salminen O, Gardner PD, Lester HA, Tapper AR.

FASEB J. 2010 Jan;24(1):49-57. doi: 10.1096/fj.09-137034. Epub 2009 Aug 31.


John Daly's compound, epibatidine, facilitates identification of nicotinic receptor subtypes.

Marks MJ, Laverty DS, Whiteaker P, Salminen O, Grady SR, McIntosh JM, Collins AC.

J Mol Neurosci. 2010 Jan;40(1-2):96-104. doi: 10.1007/s12031-009-9264-x. Epub 2009 Aug 12.


A novel fluorescent alpha-conotoxin for the study of alpha7 nicotinic acetylcholine receptors.

Hone AJ, Whiteaker P, Christensen S, Xiao Y, Meyer EL, McIntosh JM.

J Neurochem. 2009 Oct;111(1):80-9. doi: 10.1111/j.1471-4159.2009.06299.x. Epub 2009 Jul 23.


Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.

Breining SR, Bencherif M, Grady SR, Whiteaker P, Marks MJ, Wageman CR, Lester HA, Yohannes D.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4359-63. doi: 10.1016/j.bmcl.2009.05.085. Epub 2009 May 27.


Nicotinic acetylcholine receptor alpha7 subunits with a C2 cytoplasmic loop yellow fluorescent protein insertion form functional receptors.

Murray TA, Liu Q, Whiteaker P, Wu J, Lukas RJ.

Acta Pharmacol Sin. 2009 Jun;30(6):828-41. doi: 10.1038/aps.2009.78.


Pharmacological and immunochemical characterization of alpha2* nicotinic acetylcholine receptors (nAChRs) in mouse brain.

Whiteaker P, Wilking JA, Brown RW, Brennan RJ, Collins AC, Lindstrom JM, Boulter J.

Acta Pharmacol Sin. 2009 Jun;30(6):795-804. doi: 10.1038/aps.2009.68.


The road to discovery of neuronal nicotinic cholinergic receptor subtypes.

Collins AC, Salminen O, Marks MJ, Whiteaker P, Grady SR.

Handb Exp Pharmacol. 2009;(192):85-112. doi: 10.1007/978-3-540-69248-5_4. Review.


U18666A, a cholesterol-inhibition agent, modulates human neuronal nicotinic acetylcholine receptors heterologously expressed in SH-EP1 cell line.

Zheng C, Wang MY, Liu Q, Wakui M, Whiteaker P, Lukas RJ, Wu J.

J Neurochem. 2009 Mar;108(6):1526-38. doi: 10.1111/j.1471-4159.2009.05903.x. Epub 2009 Feb 16.


In vivo activation of midbrain dopamine neurons via sensitized, high-affinity alpha 6 nicotinic acetylcholine receptors.

Drenan RM, Grady SR, Whiteaker P, McClure-Begley T, McKinney S, Miwa JM, Bupp S, Heintz N, McIntosh JM, Bencherif M, Marks MJ, Lester HA.

Neuron. 2008 Oct 9;60(1):123-36. doi: 10.1016/j.neuron.2008.09.009.


Alpha-conotoxin Arenatus IB[V11L,V16D] [corrected] is a potent and selective antagonist at rat and human native alpha7 nicotinic acetylcholine receptors.

Innocent N, Livingstone PD, Hone A, Kimura A, Young T, Whiteaker P, McIntosh JM, Wonnacott S.

J Pharmacol Exp Ther. 2008 Nov;327(2):529-37. doi: 10.1124/jpet.108.142943. Epub 2008 Jul 29. Erratum in: J Pharmacol Exp Ther. 2008 Dec;327(3):1001.


Synthesis and characterization of 125I-alpha-conotoxin ArIB[V11L;V16A], a selective alpha7 nicotinic acetylcholine receptor antagonist.

Whiteaker P, Marks MJ, Christensen S, Dowell C, Collins AC, McIntosh JM.

J Pharmacol Exp Ther. 2008 Jun;325(3):910-9. doi: 10.1124/jpet.108.136895. Epub 2008 Mar 6.


The subtypes of nicotinic acetylcholine receptors on dopaminergic terminals of mouse striatum.

Grady SR, Salminen O, Laverty DC, Whiteaker P, McIntosh JM, Collins AC, Marks MJ.

Biochem Pharmacol. 2007 Oct 15;74(8):1235-46. Epub 2007 Jul 27. Review.


Chronic nicotine cell specifically upregulates functional alpha 4* nicotinic receptors: basis for both tolerance in midbrain and enhanced long-term potentiation in perforant path.

Nashmi R, Xiao C, Deshpande P, McKinney S, Grady SR, Whiteaker P, Huang Q, McClure-Begley T, Lindstrom JM, Labarca C, Collins AC, Marks MJ, Lester HA.

J Neurosci. 2007 Aug 1;27(31):8202-18.


Nicotinic alpha5 subunit deletion locally reduces high-affinity agonist activation without altering nicotinic receptor numbers.

Brown RW, Collins AC, Lindstrom JM, Whiteaker P.

J Neurochem. 2007 Oct;103(1):204-15. Epub 2007 Jun 15.

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