Publications by authors named "Michael Breslin"

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Analgesia and peripheral c-fiber modulation by selective Na v 1.8 inhibition in rhesus.
Joshua D Vardigan, Parul S Pall, Dillon S McDevitt, ChienJung Huang, Michelle K Clements, Michael J Breslin

Pain· March 2025

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Humanized Na1.8 rats overcome cross-species potency shifts in developing novel Na1.8 inhibitors.
Dillon S McDevitt, Joshua D Vardigan, Xiaoping Zhou, Thomas W Rosahl, Heather Zhou, Michael J Breslin

Neurobiol Pain· March 2025

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2-Aminopyridines as Potent and Selective Na1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model.
Michael J Breslin, Jeffrey W Schubert, Deping Wang, Chienjung Huang, Michelle K Clements

ACS Med Chem Lett· June 2024

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Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
H Marie Loughran, Kathy M Schirripa, Anthony J Roecker, Michael J Breslin, Ling Tong

ACS Med Chem Lett· January 2024

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Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation.
Chuan Hong, Noel J Byrne, Beata Zamlynny, Srivanya Tummala, Li Xiao, Michael J Breslin

Nat Commun· February 2021

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Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.
Izzat T Raheem, Michael J Breslin, Joseph Bruno, Tamara D Cabalu, Andrew Cooke

Bioorg Med Chem Lett· February 2015

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Shaping suvorexant: application of experimental and theoretical methods for driving synthetic designs.
Georgia McGaughey, Christopher I Bayly, Christopher D Cox, John D Schreier, Michael J Breslin

J Comput Aided Mol Des· January 2014

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The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.
Sean M Smith, Jason M Uslaner, Christopher D Cox, Sarah L Huszar, Christopher E Cannon, Michael J Breslin

Neuropharmacology· January 2013

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Development of a fluorescence polarization binding assay for folate receptor.
Anna Y Kornilova, Bethany Algayer, Michael Breslin, George H Addona, Victor Uebele

Anal Biochem· January 2013

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Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Izzat T Raheem, Michael J Breslin, Christine Fandozzi, Joy Fuerst, Nicole Hill

Bioorg Med Chem Lett· September 2012

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Development of a fluorescence polarization binding assay for asialoglycoprotein receptor.
Anna Y Kornilova, Bethany Algayer, Michael Breslin, Victor Uebele

Anal Biochem· June 2012

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Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.
Paul J Coleman, John D Schreier, Christopher D Cox, Michael J Breslin, David B Whitman

ChemMedChem· March 2012

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Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia.
Christopher J Winrow, Anthony L Gotter, Christopher D Cox, Pamela L Tannenbaum, Susan L Garson, Michael J Breslin

Neuropharmacology· February 2012

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Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist.
Christopher J Winrow, Anthony L Gotter, Christopher D Cox, Scott M Doran, Pamela L Tannenbaum, Michael J Breslin

J Neurogenet· March 2011

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Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Christopher D Cox, Michael J Breslin, David B Whitman, John D Schreier, Georgia B McGaughey

J Med Chem· July 2010

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Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.
David B Whitman, Christopher D Cox, Michael J Breslin, Karen M Brashear, John D Schreier

ChemMedChem· July 2009

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Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
Christopher D Cox, Paul J Coleman, Michael J Breslin, David B Whitman, Robert M Garbaccio

J Med Chem· July 2008

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Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
Christopher D Cox, Michael J Breslin, David B Whitman, Paul J Coleman, Robert M Garbaccio

Bioorg Med Chem Lett· May 2007

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Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.
Christopher D Cox, Maricel Torrent, Michael J Breslin, Brenda J Mariano, David B Whitman

Bioorg Med Chem Lett· June 2006

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Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Christopher D Cox, Michael J Breslin, Brenda J Mariano, Paul J Coleman, Carolyn A Buser

Bioorg Med Chem Lett· April 2005

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Nonpeptide alpha V beta 3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative.
Michael J Breslin, Mark E Duggan, Wasyl Halczenko, George D Hartman, Le T Duong

Bioorg Med Chem Lett· September 2004

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Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Jiabing Wang, Michael J Breslin, Paul J Coleman, Mark E Duggan, Cecilia A Hunt

Bioorg Med Chem Lett· February 2004

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Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
John H Hutchinson, Wasyl Halczenko, Karen M Brashear, Michael J Breslin, Paul J Coleman

J Med Chem· October 2003

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Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.
Michael J Breslin, Mark E Duggan, Wasyl Halczenko, Carmen Fernandez-Metzler, Cecilia A Hunt

Bioorg Med Chem Lett· May 2003

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Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
Paul J Coleman, Karen M Brashear, Cecilia A Hunt, William F Hoffman, John H Hutchinson, Michael J Breslin

Bioorg Med Chem Lett· January 2002

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