Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Margaret J. Bradbury"'
Autor:
Rebecca R. Pick, Beth A. Fleck, Dimitri E. Grigoriadis, Sam R. J. Hoare, Margaret J. Bradbury
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 341:518-531
Corticotropin-releasing factor (CRF) receptor antagonists are under preclinical and clinical investigation for stress-related disorders. In this study the impact of receptor-ligand binding kinetics on CRF 1 receptor antagonist pharmacology was invest
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a86217285e6d988ddfc4bd504c3e809
https://doi.org/10.1124/jpet.111.188714
https://doi.org/10.1124/jpet.111.188714
Autor:
John Saunders, Zhiqiang Guo, Xin-Jun Liu, Charles Q. Huang, Colin J. Loweth, Liren Zhao, R. Scott Struthers, Margaret J. Bradbury, Yun-Fei Zhu, James W. Behan, Stephen F. Betz, Neil J. Ashweek, Zhihong O’Brien, Marion Lanier, Jenny Wen, Mi Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3845-3850
A novel series of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives were designed and synthesized as GnRH receptor antagonists. SAR studies led to a series of highly active molecules against both the rat and human receptors.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::994be87ff74fc1edceedd710e1f1d8ed
https://doi.org/10.1016/j.bmcl.2007.05.009
https://doi.org/10.1016/j.bmcl.2007.05.009
Autor:
Mark A. Varney, Nicholas D. P. Cosford, Jeffery J. Anderson, Una Campbell, Margaret J. Bradbury, Deborah F. Chapman, Lida R. Tehrani, Darlene R. Giracello, Christopher D. King, A. M. Strack
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 313:395-402
The metabotropic glutamate receptor subtype mGlu5 modulates central reward pathways. Many transmitter systems within reward pathways affect feeding. We examined the potential role of mGlu5 in body weight regulation using genetic and pharmacological a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52454c9bcd6cc70440ef92af9dbd726a
https://doi.org/10.1124/jpet.104.076406
https://doi.org/10.1124/jpet.104.076406
Autor:
Jeffery J. Anderson, Mark A. Varney, Christopher D. King, Margaret J. Bradbury, Deborah F. Chapman, Greg Holtz, Nicholas D. P. Cosford, Jeffrey R. Roppe, Darlene R. Giracello
Publikováno v:
European Journal of Pharmacology. 473:35-40
In vivo receptor occupancy of mGlu5 receptor antagonists was quantified in rat and mouse brain using the mGlu5 receptor selective antagonist [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine) ([3H]methoxy-PEPy). Administration of [3H]methoxy-PEPy (50 mic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9be033af1806d2538cfdab7fc5078019
https://doi.org/10.1016/s0014-2999(03)01935-6
https://doi.org/10.1016/s0014-2999(03)01935-6
Autor:
Darlene R. Giracello, Blake A. Rowe, Nicholas D. P. Cosford, Mark A. Varney, Deborah F. Chapman, Margaret J. Bradbury, Jeffery J. Anderson, Lida R. Tehrani, Greg Holtz, Sara P. Rao
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 303:1044-1051
The binding of [3H]methoxymethyl-3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (methoxymethyl-MTEP), a potent and selective antagonist for metabotropic glutamate (mGlu)5 receptors, was characterized in rat brain both in vitro and in vivo. Nonspecifi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02261e288431280fa923c3e0993cf6e7
https://doi.org/10.1124/jpet.102.040618
https://doi.org/10.1124/jpet.102.040618
Publikováno v:
Endocrinology. 141:2715-2724
Intracerebroventricular injection of CRF or urocortin (Ucn) reduces appetite and body weight. CRFR1 and CRFR2, the receptors for CRF and Ucn, are expressed in neurons associated with appetite-control and metabolism, but their relative contributions i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21693169a761788d3a5eca73d9fd63ab
https://doi.org/10.1210/endo.141.8.7606
https://doi.org/10.1210/endo.141.8.7606
Publikováno v:
Endocrinology. 141:2285-2293
CRF receptor type 2 (CRF R2) messenger RNA (mRNA) expression in the rodent heart is modulated by exposure to both the bacterial endotoxin lipopolysaccharide (LPS) and glucocorticoids. In this study we examined the roles of glucocorticoids, cytokines,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::825b71a52ddd4891b5822448cf865d4c
https://doi.org/10.1210/endo.141.7.7572
https://doi.org/10.1210/endo.141.7.7572
Publikováno v:
Endocrinology. 140:5651-5658
Urocortin (Ucn), a new mammalian member of the CRF family, is a candidate endogenous ligand for type 2 CRF receptors. In a survey of peripheral tissues from adult male rats, we found that Ucn messenger RNA (mRNA) was abundant in the gastrointestinal
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::10f0156738d1d13e69bc5fcfb9377cfc
https://doi.org/10.1210/endo.140.12.7223
https://doi.org/10.1210/endo.140.12.7223
Autor:
Sam R. J. Hoare, Graham Beaton, Bin-Feng Li, Paul D. Crowe, Said Zamani-Kord, Lisa M. Hernández, Wilna J. Moree, Charles Q. Huang, Jinghua Yu, Hua Wang, Siobhan Malany, Fabio C. Tucci, Chun Yang, Ajay Madan, Aida Sacaan, Robert E. Petroski, Jianyun Wen, Coon Timothy Richard, Margaret J. Bradbury, Kayvon Jalali, Dragan Marinkovic
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(19)
Analogs of the known H(1)-antihistamine R-dimethindene with suitable selectivity for key GPCRs, P450 enzymes and hERG channel were assessed for metabolism profile and in vivo properties. Several analogs were determined to exhibit diverse metabolism.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::27771b1fadd5556d09bba470020874b2
https://pubmed.ncbi.nlm.nih.gov/20800486
https://pubmed.ncbi.nlm.nih.gov/20800486
Autor:
Coon Timothy Richard, Raymond S. Gross, Siobhan Malany, Florence Jovic, Wilna J. Moree, Zhihong O’Brien, Sam R. J. Hoare, Paul D. Crowe, Fabio C. Tucci, Bin-Feng Li, Graham Beaton, Margaret J. Bradbury, Hua Wang, Jianyun Wen, Robert E. Petroski, Jinghua Yu, Aida Sacaan, Dragan Marinkovic, Lisa M. Hernández, Ajay Madan
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
SAR of lead benzothiophene H1-antihistamine 2 was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-lives in humans wer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3dc05606f54d1888dffbf938419ff93
https://pubmed.ncbi.nlm.nih.gov/20188547
https://pubmed.ncbi.nlm.nih.gov/20188547