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Items: 29

1.

Synthesis and evaluation of new radioligands [(11)C]A-833834 and [(11)C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors.

Horti AG, Ravert HT, Gao Y, Holt DP, Bunnelle WH, Schrimpf MR, Li T, Ji J, Valentine H, Scheffel U, Kuwabara H, Wong DF, Dannals RF.

Nucl Med Biol. 2013 Apr;40(3):395-402. doi: 10.1016/j.nucmedbio.2012.11.013. Epub 2013 Jan 5.

2.

SAR of α7 nicotinic receptor agonists derived from tilorone: exploration of a novel nicotinic pharmacophore.

Schrimpf MR, Sippy KB, Briggs CA, Anderson DJ, Li T, Ji J, Frost JM, Surowy CS, Bunnelle WH, Gopalakrishnan M, Meyer MD.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1633-8. doi: 10.1016/j.bmcl.2011.12.126. Epub 2012 Jan 8.

PMID:
22281189
3.

Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.

Scanio MJ, Shi L, Bunnelle WH, Anderson DJ, Helfrich RJ, Malysz J, Thorin-Hagene KK, Van Handel CE, Marsh KC, Lee CH, Gopalakrishnan M.

J Med Chem. 2011 Nov 10;54(21):7678-92. doi: 10.1021/jm201045m. Epub 2011 Oct 11.

PMID:
21962147
4.

Role of α7 nicotinic acetylcholine receptors in regulating tumor necrosis factor-α (TNF-α) as revealed by subtype selective agonists.

Li J, Mathieu SL, Harris R, Ji J, Anderson DJ, Malysz J, Bunnelle WH, Waring JF, Marsh KC, Murtaza A, Olson LM, Gopalakrishnan M.

J Neuroimmunol. 2011 Oct 28;239(1-2):37-43. doi: 10.1016/j.jneuroim.2011.08.007. Epub 2011 Sep 10.

PMID:
21911260
5.

Reagents for stereoselective preparation of N-carbamyl β-D-glucuronides.

Bunnelle WH.

J Org Chem. 2011 Jul 1;76(13):5429-32. doi: 10.1021/jo200238d. Epub 2011 Jun 6.

PMID:
21598979
6.

In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107.

Malysz J, Anderson DJ, Grønlien JH, Ji J, Bunnelle WH, Håkerud M, Thorin-Hagene K, Ween H, Helfrich R, Hu M, Gubbins E, Gopalakrishnan S, Puttfarcken PS, Briggs CA, Li J, Meyer MD, Dyhring T, Ahring PK, Nielsen EØ, Peters D, Timmermann DB, Gopalakrishnan M.

J Pharmacol Exp Ther. 2010 Sep 1;334(3):863-74. doi: 10.1124/jpet.110.167072. Epub 2010 May 26.

PMID:
20504915
7.

In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer's disease.

Bitner RS, Bunnelle WH, Decker MW, Drescher KU, Kohlhaas KL, Markosyan S, Marsh KC, Nikkel AL, Browman K, Radek R, Anderson DJ, Buccafusco J, Gopalakrishnan M.

J Pharmacol Exp Ther. 2010 Sep 1;334(3):875-86. doi: 10.1124/jpet.110.167213. Epub 2010 May 26.

PMID:
20504913
8.

Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.

Li T, Bunnelle WH, Ryther KB, Anderson DJ, Malysz J, Helfrich R, Grønlien JH, Håkerud M, Peters D, Schrimpf MR, Gopalakrishnan M, Ji J.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3636-9. doi: 10.1016/j.bmcl.2010.04.105. Epub 2010 Apr 28.

PMID:
20472430
9.

Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor.

Mortell KH, Schrimpf MR, Bunnelle WH, Anderson DJ, Gronlien JH, Hagene KT, Gopalakrishnan M.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):104-7. doi: 10.1016/j.bmcl.2009.11.023. Epub 2009 Nov 14.

PMID:
19954975
10.

Role of channel activation in cognitive enhancement mediated by alpha7 nicotinic acetylcholine receptors.

Briggs CA, Grønlien JH, Curzon P, Timmermann DB, Ween H, Thorin-Hagene K, Kerr P, Anderson DJ, Malysz J, Dyhring T, Olsen GM, Peters D, Bunnelle WH, Gopalakrishnan M.

Br J Pharmacol. 2009 Nov;158(6):1486-94. doi: 10.1111/j.1476-5381.2009.00426.x. Epub 2009 Oct 20.

11.

Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.

Bunnelle WH, Tietje KR, Frost JM, Peters D, Ji J, Li T, Scanio MJ, Shi L, Anderson DJ, Dyhring T, Grønlien JH, Ween H, Thorin-Hagene K, Meyer MD.

J Med Chem. 2009 Jul 23;52(14):4126-41. doi: 10.1021/jm900249k.

PMID:
19552432
12.

Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.

Faghih R, Gopalakrishnan SM, Gronlien JH, Malysz J, Briggs CA, Wetterstrand C, Ween H, Curtis MP, Sarris KA, Gfesser GA, El-Kouhen R, Robb HM, Radek RJ, Marsh KC, Bunnelle WH, Gopalakrishnan M.

J Med Chem. 2009 May 28;52(10):3377-84. doi: 10.1021/jm9003818.

PMID:
19419141
13.

In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.

Malysz J, Grønlien JH, Anderson DJ, Håkerud M, Thorin-Hagene K, Ween H, Wetterstrand C, Briggs CA, Faghih R, Bunnelle WH, Gopalakrishnan M.

J Pharmacol Exp Ther. 2009 Jul;330(1):257-67. doi: 10.1124/jpet.109.151886. Epub 2009 Apr 23.

PMID:
19389923
14.

Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.

Sippy KB, Anderson DJ, Bunnelle WH, Hutchins CW, Schrimpf MR.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1682-5. doi: 10.1016/j.bmcl.2009.01.099. Epub 2009 Feb 4.

PMID:
19232492
15.

Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties.

Tietje KR, Anderson DJ, Bitner RS, Blomme EA, Brackemeyer PJ, Briggs CA, Browman KE, Bury D, Curzon P, Drescher KU, Frost JM, Fryer RM, Fox GB, Gronlien JH, Håkerud M, Gubbins EJ, Halm S, Harris R, Helfrich RJ, Kohlhaas KL, Law D, Malysz J, Marsh KC, Martin RL, Meyer MD, Molesky AL, Nikkel AL, Otte S, Pan L, Puttfarcken PS, Radek RJ, Robb HM, Spies E, Thorin-Hagene K, Waring JF, Ween H, Xu H, Gopalakrishnan M, Bunnelle WH.

CNS Neurosci Ther. 2008 Spring;14(1):65-82. doi: 10.1111/j.1527-3458.2008.00037.x. Review.

16.

alpha7 nicotinic acetylcholine receptor agonist properties of tilorone and related tricyclic analogues.

Briggs CA, Schrimpf MR, Anderson DJ, Gubbins EJ, Grønlien JH, Håkerud M, Ween H, Thorin-Hagene K, Malysz J, Li J, Bunnelle WH, Gopalakrishnan M, Meyer MD.

Br J Pharmacol. 2008 Mar;153(5):1054-61. Epub 2007 Dec 24.

17.

[3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic receptor agonist: radioligand binding characterization to rat and human brain.

Anderson DJ, Bunnelle W, Surber B, Du J, Surowy C, Tribollet E, Marguerat A, Bertrand D, Gopalakrishnan M.

J Pharmacol Exp Ther. 2008 Jan;324(1):179-87. Epub 2007 Oct 24.

PMID:
17959745
18.

Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists.

Ji J, Schrimpf MR, Sippy KB, Bunnelle WH, Li T, Anderson DJ, Faltynek C, Surowy CS, Dyhring T, Ahring PK, Meyer MD.

J Med Chem. 2007 Nov 1;50(22):5493-508. Epub 2007 Oct 11.

PMID:
17929796
19.

Broad-spectrum efficacy across cognitive domains by alpha7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathways.

Bitner RS, Bunnelle WH, Anderson DJ, Briggs CA, Buccafusco J, Curzon P, Decker MW, Frost JM, Gronlien JH, Gubbins E, Li J, Malysz J, Markosyan S, Marsh K, Meyer MD, Nikkel AL, Radek RJ, Robb HM, Timmermann D, Sullivan JP, Gopalakrishnan M.

J Neurosci. 2007 Sep 26;27(39):10578-87.

20.

A-366833: a novel nicotinonitrile-substituted 3,6-diazabicyclo[3.2.0]-heptane alpha4beta2 nicotinic acetylcholine receptor selective agonist: Synthesis, analgesic efficacy and tolerability profile in animal models.

Ji J, Bunnelle WH, Anderson DJ, Faltynek C, Dyhring T, Ahring PK, Rueter LE, Curzon P, Buckley MJ, Marsh KC, Kempf-Grote A, Meyer MD.

Biochem Pharmacol. 2007 Oct 15;74(8):1253-62. Epub 2007 Aug 12.

PMID:
17854775
21.

Structure-activity studies and analgesic efficacy of N-(3-pyridinyl)-bridged bicyclic diamines, exceptionally potent agonists at nicotinic acetylcholine receptors.

Bunnelle WH, Daanen JF, Ryther KB, Schrimpf MR, Dart MJ, Gelain A, Meyer MD, Frost JM, Anderson DJ, Buckley M, Curzon P, Cao YJ, Puttfarcken P, Searle X, Ji J, Putman CB, Surowy C, Toma L, Barlocco D.

J Med Chem. 2007 Jul 26;50(15):3627-44. Epub 2007 Jun 22.

PMID:
17585748
22.

Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists.

Frost JM, Bunnelle WH, Tietje KR, Anderson DJ, Rueter LE, Curzon P, Surowy CS, Ji J, Daanen JF, Kohlhaas KL, Buckley MJ, Henry RF, Dyhring T, Ahring PK, Meyer MD.

J Med Chem. 2006 Dec 28;49(26):7843-53.

PMID:
17181167
23.

(L)-Phenylglycine, but not necessarily other alpha2delta subunit voltage-gated calcium channel ligands, attenuates neuropathic pain in rats.

Lynch JJ 3rd, Honore P, Anderson DJ, Bunnelle WH, Mortell KH, Zhong C, Wade CL, Zhu CZ, Xu H, Marsh KC, Lee CH, Jarvis MF, Gopalakrishnan M.

Pain. 2006 Nov;125(1-2):136-42. Epub 2006 Jun 14.

PMID:
16781071
24.

A-186253, a specific antagonist of the alpha 4 beta 2 nAChRs: its properties and potential to study brain nicotinic acetylcholine receptors.

Itier V, Schönbächler R, Tribollet E, Honer M, Prinz K, Marguerat A, Bertrand S, Bunnelle WH, Schubiger PA, Meyer MD, Sullivan JP, Bertrand D, Westera G.

Neuropharmacology. 2004 Sep;47(4):538-57.

PMID:
15380372
25.

Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.

Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP.

J Med Chem. 2004 Jun 3;47(12):3220-35.

PMID:
15163201
26.

Design of ligands for the nicotinic acetylcholine receptors: the quest for selectivity.

Bunnelle WH, Dart MJ, Schrimpf MR.

Curr Top Med Chem. 2004;4(3):299-334. Review.

PMID:
14754449
27.

Selective amination of polyhalopyridines catalyzed by a palladium-xantphos complex.

Ji J, Li T, Bunnelle WH.

Org Lett. 2003 Nov 27;5(24):4611-4.

PMID:
14627396
28.

Synthesis and biological evaluation of pyridine-modified analogues of 3-(2-aminoethoxy)pyridine as novel nicotinic receptor ligands.

Lin NH, Dong L, Bunnelle WH, Anderson DJ, Meyer MD.

Bioorg Med Chem Lett. 2002 Nov 18;12(22):3321-4.

PMID:
12392742
29.

6-Chloropyridazin-3-yl derivatives active as nicotinic agents: synthesis, binding, and modeling studies.

Toma L, Quadrelli P, Bunnelle WH, Anderson DJ, Meyer MD, Cignarella G, Gelain A, Barlocco D.

J Med Chem. 2002 Aug 29;45(18):4011-7.

PMID:
12190322

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