Publications by authors named "Stacy Markison"

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Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist.
Sun Hee Kim, Sangdon Han, Jian Zhao, Shimiao Wang, Ana Karin Kusnetzow, Stacy Markison

ACS Med Chem Lett· April 2024

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Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist.
Jian Zhao, Shimiao Wang, Stacy Markison, Sun Hee Kim, Sangdon Han

ACS Med Chem Lett· January 2023

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Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Jian Zhao, Shimiao Wang, Sun Hee Kim, Sangdon Han, Elizabeth Rico-Bautista, Stacy Markison

Bioorg Med Chem Lett· September 2022

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Paltusotine, a novel oral once-daily nonpeptide SST2 receptor agonist, suppresses GH and IGF-1 in healthy volunteers.
Ajay Madan, Stacy Markison, Stephen F Betz, Alan Krasner, Rosa Luo

Pituitary· April 2022

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Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1-1,2,4-triazol-5-yl)thio)methyl)pyridine.
Donald S Karanewsky, Amy J Arthur, Hanghui Liu, Bert Chi, Lily Ida, Stacy Markison

Toxicol Rep· May 2016

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Toxicological evaluation of two novel bitter modifying flavour compounds: 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1-pyrazol-4-yl)-1-(3-hydroxybenzyl)imidazolidine-2,4-dione and 3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1-pyrazol-4-yl)-1-(3-hydroxybenzyl)-5,5-dimethylimidazolidine-2,4-dione.
Donald S Karanewsky, Amy J Arthur, Hanghui Liu, Bert Chi, Lily Ida, Stacy Markison

Toxicol Rep· February 2016

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Toxicological evaluation of the flavour ingredient 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid.
Amy J Arthur, Donald S Karanewsky, Hanghui Liu, Bert Chi, Stacy Markison

Toxicol Rep· September 2015

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Toxicological evaluation of a novel cooling compound: 2-(4-methylphenoxy)--(1-pyrazol-3-yl)--(2-thienylmethyl)acetamide.
Donald S Karanewsky, Amy J Arthur, Hanghui Liu, Bert Chi, Stacy Markison

Toxicol Rep· September 2015

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N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.
Marion C Lanier, Manisha Moorjani, Zhiyong Luo, Yongsheng Chen, Emily Lin, Stacy Markison

J Med Chem· February 2009

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Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.
Xiaohu Zhang, John E Tellew, Zhiyong Luo, Manisha Moorjani, Emily Lin, Stacy Markison

J Med Chem· November 2008

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Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Chen Chen, Fabio C Tucci, Wanlong Jiang, Joe A Tran, Beth A Fleck, Stacy Markison

Bioorg Med Chem· May 2008

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2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.
Deborah H Slee, Yongsheng Chen, Xiaohu Zhang, Manisha Moorjani, Marion C Lanier, Stacy Markison

J Med Chem· March 2008

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2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Deborah H Slee, Manisha Moorjani, Xiaohu Zhang, Emily Lin, Marion C Lanier, Stacy Markison

J Med Chem· March 2008

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Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Xiaohu Zhang, Jaimie K Rueter, Yongsheng Chen, Manisha Moorjani, Marion C Lanier, Stacy Markison

Bioorg Med Chem Lett· March 2008

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Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Deborah H Slee, Xiaohu Zhang, Manisha Moorjani, Emily Lin, Marion C Lanier, Stacy Markison

J Med Chem· February 2008

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Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.
Chen Chen, Wanlong Jiang, Joe A Tran, Fabio C Tucci, Beth A Fleck, Stacy Markison

Bioorg Med Chem Lett· January 2008

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Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.
Wanlong Jiang, Joe A Tran, Fabio C Tucci, Beth A Fleck, Sam R Hoare, Stacy Markison

Bioorg Med Chem Lett· December 2007

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Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Joe A Tran, Wanlong Jiang, Fabio C Tucci, Beth A Fleck, Jenny Wen, Stacy Markison

J Med Chem· December 2007

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Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Chen Chen, Wanlong Jiang, Fabio Tucci, Joe A Tran, Beth A Fleck, Stacy Markison

J Med Chem· November 2007

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Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Wanlong Jiang, Fabio C Tucci, Joe A Tran, Beth A Fleck, Jenny Wen, Stacy Markison

Bioorg Med Chem Lett· October 2007

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Peripheral administration of the melanocortin-4 receptor antagonist NBI-12i ameliorates uremia-associated cachexia in mice.
Wai W Cheung, Huey-Ju Kuo, Stacy Markison, Chen Chen, Alan C Foster

J Am Soc Nephrol· September 2007

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Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Joe A Tran, Fabio C Tucci, Wanlong Jiang, Dragan Marinkovic, Caroline W Chen, Stacy Markison

Bioorg Med Chem· August 2007

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A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.
Brian Dyck, Stacy Markison, Liren Zhao, Junko Tamiya, Jonathan Grey

J Med Chem· June 2006

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Molecular interactions of nonpeptide agonists and antagonists with the melanocortin-4 receptor.
Beth A Fleck, Chen Chen, Weidong Yang, Rajesh Huntley, Stacy Markison

Biochemistry· November 2005

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Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines.
Fabio C Tucci, Nicole S White, Stacy Markison, Margaret Joppa, Joe A Tran

Bioorg Med Chem Lett· October 2005

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