Publications by authors named "Ryan Westphal"

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Discovery of pyrrolo[2,1-][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain.
Carolyn D Dzierba, Bireshwar Dasgupta, George Karageorge, Walter Kostich, Brian Hamman, Ryan Westphal

Med Chem Res· June 2023

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The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu PAM development candidate.
Joseph D Panarese, Darren W Engers, Yong-Jin Wu, Jason M Guernon, Aspen Chun, Ryan Westphal

Bioorg Med Chem Lett· January 2019

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The Novel, Nicotinic Alpha7 Receptor Partial Agonist, BMS-933043, Improves Cognition and Sensory Processing in Preclinical Models of Schizophrenia.
Linda J Bristow, Amy E Easton, Yu-Wen Li, Digavalli V Sivarao, Regina Lidge, Ryan Westphal

PLoS One· August 2017

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Effects of BMS-902483, an α7 nicotinic acetylcholine receptor partial agonist, on cognition and sensory gating in relation to receptor occupancy in rodents.
Rick L Pieschl, Regina Miller, Kelli M Jones, Debra J Post-Munson, Ping Chen, Ryan S Westphal

Eur J Pharmacol· July 2017

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BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
Dalton King, Christiana Iwuagwu, Jim Cook, Ivar M McDonald, Robert Mate, Ryan Westphal

ACS Med Chem Lett· March 2017

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Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.
Andrew P Degnan, Darrell Maxwell, Anand Balakrishnan, Jeffrey M Brown, Amy Easton, Ryan Westphal

Bioorg Med Chem Lett· December 2016

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Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
Walter Kostich, Brian D Hamman, Yu-Wen Li, Sreenivasulu Naidu, Kumaran Dandapani, Ryan Westphal

J Pharmacol Exp Ther· September 2016

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Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.
Hong Huang, Andrew P Degnan, Anand Balakrishnan, Amy Easton, Michael Gulianello, Ryan Westphal

Bioorg Med Chem Lett· September 2016

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Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.
Louis S Chupak, Xiaofan Zheng, Shuanghua Hu, Yazhong Huang, Min Ding, Ryan S Westphal

Bioorg Med Chem· April 2016

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Biochemical and behavioral effects of PDE10A inhibitors: Relationship to target site occupancy.
Yu-Wen Li, Matthew A Seager, Trevor Wojcik, Karen Heman, Thaddeus F Molski, Ryan Westphal

Neuropharmacology· March 2016

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Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.
Fukang Yang, Lawrence B Snyder, Anand Balakrishnan, Jeffrey M Brown, Digavalli V Sivarao, Ryan Westphal

ACS Med Chem Lett· March 2016

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Evidence for Classical Cholinergic Toxicity Associated with Selective Activation of M1 Muscarinic Receptors.
Andrew Alt, Annapurna Pendri, Robert L Bertekap, Guo Li, Yulia Benitex, Ryan S Westphal

J Pharmacol Exp Ther· February 2016

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Discovery of D1 Dopamine Receptor Positive Allosteric Modulators: Characterization of Pharmacology and Identification of Residues that Regulate Species Selectivity.
Martin A Lewis, Lisa Hunihan, John Watson, Robert G Gentles, Shuanghua Hu, Ryan S Westphal

J Pharmacol Exp Ther· September 2015

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Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
Carolyn D Dzierba, Yingzhi Bi, Bireshwar Dasgupta, Richard A Hartz, Vijay Ahuja, Ryan Westphal

Bioorg Med Chem Lett· April 2015

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The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.
Yingzhi Bi, Carolyn D Dzierba, Cynthia Fink, Yudith Garcia, Michael Green, Ryan S Westphal

Bioorg Med Chem Lett· April 2015

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Identification of small molecules that selectively inhibit diacylglycerol lipase-α activity.
Kingsley K Appiah, Yuval Blat, Barbara J Robertson, Bradley C Pearce, Donna L Pedicord, Ryan S Westphal

J Biomol Screen· April 2014

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In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10).
Jeffrey M Brown, Lisa Hunihan, Margaret M Prack, David G Harden, Joanne Bronson, Ryan S Westphal

J Neurochem· April 2014

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Structure activity relationship studies of 3-arylsulfonyl-pyrido[1,2-a]pyrimidin-4-imines as potent 5-HT₆ antagonists.
Shuanghua Hu, Yazhong Huang, Yong-Jin Wu, Huan He, Katherine A Grant-Young, Ryan S Westphal

Bioorg Med Chem· March 2014

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Discovery of a cyclopentylamine as an orally active dual NK1 receptor antagonist-serotonin reuptake transporter inhibitor.
Yong-Jin Wu, Huan He, Qi Gao, Dedong Wu, Robert Bertekap, Ryan S Westphal

Bioorg Med Chem Lett· March 2014

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Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Yong-Jin Wu, Huan He, Robert Bertekap, Ryan Westphal, Snjezana Lelas

Bioorg Med Chem· April 2013

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Design of an automated enhanced-throughput platform for functional characterization of positive allosteric modulator-induced leftward shifts in apparent agonist potency in vitro.
Adam Hendricson, Michele Matchett, Meredith Ferrante, Chris Ferrante, Ed Hunnicutt, Ryan Westphal

J Lab Autom· April 2012

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Postsynaptic diacylglycerol lipase mediates retrograde endocannabinoid suppression of inhibition in mouse prefrontal cortex.
Hiroki Yoshino, Takeaki Miyamae, Gwenn Hansen, Brian Zambrowicz, Michael Flynn, Ryan S Westphal

J Physiol· October 2011

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Small molecule receptor protein tyrosine phosphatase γ (RPTPγ) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.
Steven Sheriff, Brett R Beno, Weixu Zhai, Walter A Kostich, Patricia A McDonnell, Ryan S Westphal

J Med Chem· October 2011

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Molecular characterization and identification of surrogate substrates for diacylglycerol lipase α.
Donna L Pedicord, Michael J Flynn, Caroline Fanslau, Maricar Miranda, Lisa Hunihan, Ryan S Westphal

Biochem Biophys Res Commun· August 2011

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Cloning, purification, crystallization and preliminary X-ray analysis of the catalytic domain of human receptor-like protein tyrosine phosphatase γ in three different crystal forms.
Kevin Kish, Patricia A McDonnell, Valentina Goldfarb, Mian Gao, William J Metzler, Ryan S Westphal

Acta Crystallogr Sect F Struct Biol Cryst Commun· July 2011

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