Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Margaret Joppa"'
Autor:
Michael Johns, Beth A. Fleck, Ajay Madan, Dragan Marinkovic, Margaret Joppa, Chen Chen, Stacy Markison, Wanlong Jiang, Melissa Arellano, Alan C. Foster, Joe A. Tran, Fabio C. Tucci, Takung Chen, Jenny Wen, Yang Sai, Sam R. J. Hoare, Caroline W. Chen, John Saunders
Publikováno v:
Journal of Medicinal Chemistry. 50:5249-5252
A potent and selective antagonist of the melanocortin-4 receptor, 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-6-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)propionyl]piperazine (10d), was identified from a series piperazinebenzylami
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbb47533ec95478689b130f37e9c0174
https://doi.org/10.1021/jm070806a
https://doi.org/10.1021/jm070806a
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
https://doi.org/10.1016/j.peptides.2005.03.002
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
https://doi.org/10.1016/j.bmcl.2005.06.071
Publikováno v:
Peptides. 28(3)
Cachexia is a clinical wasting syndrome that occurs in multiple disease states, and is associated with anorexia and a progressive loss of body fat and lean mass. The development of new therapeutics for this disorder is needed due to poor efficacy and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bb6c83a083b8e517e028026779a10e9e
https://pubmed.ncbi.nlm.nih.gov/17204351
https://pubmed.ncbi.nlm.nih.gov/17204351
Autor:
Melissa Arellano, Fabio C. Tucci, Alan C. Foster, Stacy Markison, Chen Chen, Beth A. Fleck, John Saunders, Marion Lanier, Joseph Pontillo, Dragan Marinkovic, Joseph A. Tran, Sam R. J. Hoare, Margaret Joppa, Jodie Nelson
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(10)
Optimization on a series of piperazinebenzylamines resulted in analogues with low nanomolar binding at the human MC4 receptor but weak affinity (Ki > 500 nM) at the MC3 receptor. Compound 14c was identified to be a potent MC4R antagonist (Ki = 3.2 nM
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8dd4aad8bf20b143baaae38980fdef3
https://pubmed.ncbi.nlm.nih.gov/15863313
https://pubmed.ncbi.nlm.nih.gov/15863313
Autor:
Raymond S. Gross, Haig Bozigian, Mary Jane Cullen, Mary Ann Pelleymounter, Dacie Lewis, Ta Kung Chen, Alan C. Foster, Margaret Joppa, Kathleen Gogas
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 311(2)
Indiplon (NBI 34060; N-methyl-N-[3-[3-(2-thienylcarbonyl)-pyrazolo[1,5-alpha]pyrimidin-7-yl]phenyl]acetamide), a novel pyrazolopyrimidine and high-affinity allosteric potentiator of GABA(A) receptor function, was profiled for its effects in rodents a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bab0b5cdf37209c5ae3412ca4601bb4
https://pubmed.ncbi.nlm.nih.gov/15256538
https://pubmed.ncbi.nlm.nih.gov/15256538
Publikováno v:
Peptides. 25(4)
We compared the in vivo efficacy of two selective CRF2 agonists, mouse urocortin II (mUcn II) and human urocortin III (hUcn III), using food intake, anxious behavior, or ACTH release in CD-1 or Balb/c mice as indices of biological stress responses. A
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00c246d0a86502cde604a9cd3af4e3a1
https://pubmed.ncbi.nlm.nih.gov/15165722
https://pubmed.ncbi.nlm.nih.gov/15165722
Autor:
Alan C. Foster, Meira Wolff, John Saunders, Margaret Joppa, Stacy Markison, Mary J. Cismowski, Paul J. Conlon, Val S. Goodfellow, Beth A. Fleck, Brian J. Murphy, Chen Chen, Nicholas Ling, Kathy R. Gogas
Publikováno v:
Annals of the New York Academy of Sciences. 994
There has been great interest in melanocortin (MC) receptors as targets for the design of novel therapeutics to treat disorders of body weight, such as obesity and cachexia. Both genetic and pharmacological evidence points toward central MC4 receptor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc6a9f37b6837c12a52cae0c10a69de5
https://pubmed.ncbi.nlm.nih.gov/12851304
https://pubmed.ncbi.nlm.nih.gov/12851304
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 302(1)
Corticotropin-releasing factor (CRF) is one of the principle components of the stress response. The physiological effects of CRF are mediated by two receptor subtypes, CRF(1) and CRF(2). Recent data obtained with the selective CRF(2) antagonist antis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9583d5f3d5fc252dd5f7adb96c35efd3
https://pubmed.ncbi.nlm.nih.gov/12065711
https://pubmed.ncbi.nlm.nih.gov/12065711
Autor:
Margaret Joppa, Stephen C. Heinrichs, Rick Nelson, Jeannette Lapsansky, Karen Jeske, Errol B. De Souza
Publikováno v:
Physiologybehavior. 74(1-2)
Acute administration of corticotropin-releasing factor (CRF) results in anorexic and sympathomimetic effects that suggest efficacy in chronic models of energy balance. The present studies employed a broad spectrum energy balance indices in lean and g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::257732285846b07016e0949f908ec8b1
https://pubmed.ncbi.nlm.nih.gov/11564446
https://pubmed.ncbi.nlm.nih.gov/11564446