Výsledky vyhledávání - "Kathleen Gogas"

NKTR-181: A Novel Mu-Opioid Analgesic with Inherently Low Abuse Potential

Autor: Stephen K. Doberstein, Phi Quach, Kathleen Gogas, Takahiro Miyazaki, Daniel McWeeney, Irene Y. Choi, Jennifer A. Riggs, David Gauvin, Juli Evans, Cherie F. Ali, Juergen W. Pfeiffer, Jonathan Zalevsky, Werner Rubas, Timothy A. Riley, Neel K. Anand, Hema Gursahani, Marlene Hennessy, Grace Kim

Publikováno v: The Journal of pharmacology and experimental therapeutics. 363(1)

The increasing availability of prescription opioid analgesics for the treatment of pain has been paralleled by an epidemic of opioid misuse, diversion, and overdose. The development of abuse-deterrent formulations (ADFs) of conventional opioids such

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b60ec3d5b31fa337024f90b96e69d05a
https://pubmed.ncbi.nlm.nih.gov/28778859

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Synthesis and structure–activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics

Autor: Joseph Pontillo, Hua Wang, Beth A. Fleck, Warren Wade, Dongpei Wu, Sarah Hudson, Marc J. Genicot, Brett Ching, Kathleen Gogas, Anna Aparicio, Jenny Wen, Yinghong Gao, Todd Ewing

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:6151-6155

The design synthesis and SAR of a series of chiral ring-constrained norepinephrine reuptake inhibitors with improved physicochemical properties is described. Typical compounds are potent (IC(50)s10 nM), selective against the other monoamine transport

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3f1023a9ba26c4a0051e002f2b4f2ea
https://doi.org/10.1016/j.bmcl.2008.10.013

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Structure–activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability

Autor: Anna Aparicio, Sarah Hudson, Warren Wade, Hua Wang, Wesley J. Dwight, Yalda S. Mostofi, Wendy Eccles, Jenny Wen, Mehrak Kiankarimi, Kathleen Gogas, Beth A. Fleck, Marc J. Genicot

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:4491-4494

The synthesis and SAR of a series of chiral heterocyclic ring-constrained norepinephrine reuptake inhibitors are described. The best compounds compare favorably with atomoxetine in potency (IC(50)s10 nM), selectivity against the other monoamine trans

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7dd576616be21f774ec8d52ceb4b4a7d
https://doi.org/10.1016/j.bmcl.2008.07.049

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Glutamate-based therapeutic approaches: NR2B receptor antagonists

Autor: Kathleen Gogas

Publikováno v: Current Opinion in Pharmacology. 6:68-74

Over the past decade, there have been major advances in our understanding of the role of glutamate and N-methyl-d-aspartate (NMDA) receptors in several disorders of the central nervous system, including stroke, Parkinson's disease, Huntington's disea

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3448788946f5a645aa50eef4a095618e
https://doi.org/10.1016/j.coph.2005.11.001

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Central administration of peptide and small molecule MC4 receptor antagonists induce hyperphagia in mice and attenuate cytokine-induced anorexia

Autor: Alan C. Foster, Stacy Markison, Nick Ling, Margaret Joppa, Kathleen Gogas, Caroline W. Chen

Publikováno v: Peptides. 26:2294-2301

We investigated the effect of melanocortin 4 receptor (MC4) antagonists on food intake in mice. Food intake during the light phase was significantly increased by ICV administration of mixed MC3/MC4 antagonists (AgRP and SHU9119) or MC4 selective anta

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60f8de05bac65de18651d203f65a5db9
https://doi.org/10.1016/j.peptides.2005.03.002

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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

Autor: Dragan Marinkovic, Val S. Goodfellow, Stacy Markison, Jessica Parker, Alan C. Foster, Joseph Pontillo, L. Melissa Arellano, Beth A. Fleck, Nicole S. White, Margaret Joppa, Wanlong Jiang, Joe A. Tran, Caroline W. Chen, Kathleen Gogas, Fabio C. Tucci, Ajay Madan, Chen Chen, John Saunders, Brian Dyck

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 15:4389-4395

The melanocortin-4 receptor (MC4R) plays an important role in the regulation of energy homeostasis. Recent studies have shown that blockade of the MC4R reverses tumor-induced weight loss in mice. Herein, we describe the synthesis and identification o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7198023fd4efbda4dcdb0af459fe067
https://doi.org/10.1016/j.bmcl.2005.06.071

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1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists

Autor: Mingzhu Zhang, David A. Schwarz, Tracy Baker, Val S. Goodfellow, Kathleen Gogas, Stacy Markison, Christopher E. Heise, Xiaochuan Wang, Yun-Fei Zhu, Charles Q. Huang, Takung Chen, Jun Fan

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 15:3701-3706

Derivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine were identified as potent and functionally active MCH-R1 antagonists. One compound with Ki = 2.3 nM demonstrated good oral bioavailability (32%

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1561713df671ea102232829150e9771
https://doi.org/10.1016/j.bmcl.2005.05.130

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Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint

Autor: Sarah Hudson, Mehrak Kiankarimi, Wesley J. Dwight, Warren Wade, Kathleen Gogas, Yalda S. Mostofi, Beth A. Fleck, Wendy Eccles, Marc J. Genicot

Publikováno v: Bioorganicmedicinal chemistry letters. 18(16)

The design, synthesis and SAR of a series of heterocyclic ring-constrained norepinephrine reuptake inhibitors are described. As racemates, the best compounds compare favorably with atomoxetine (IC(50)'s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98dd54c253e9b6994fbfdfc72c6e6c31
https://pubmed.ncbi.nlm.nih.gov/18667309

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Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI)

Autor: Kathleen Gogas, Warren Wade, Dongpei Wu, Sarah Hudson, Brett Ching, Joseph Pontillo, Beth A. Fleck, Yinghong Gao

Publikováno v: Bioorganicmedicinal chemistry letters. 18(14)

The design, synthesis, and SAR of a series of ring-constrained norepinephrine reuptake inhibitors are described. A substantially rigid inhibitor with potent functional activity at the transporter (IC(50)=8 nM) was used to develop a model for the dist

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::257dd6dcb0f5b0c3ec9219aadde4906e
https://pubmed.ncbi.nlm.nih.gov/18550369

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Anxiety

Autor: Sandra M. Lechner, John P. Williams, Kathleen Gogas, W. McCarthy, Dimitri E. Grigoriadis, Alan C. Foster, Stacy Markison

Anxiety is an integral part of life. Most individuals have experienced mild anxiety when preparing for a big event e. g., giving a lecture or taking an exam. In these situations, anxiety is beneficial, leading to heightened alertness and preparation

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bbbcf7598a1c6706d31c20f6b3c62dda
https://doi.org/10.1016/b0-08-045044-x/00164-4

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