Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Gilbert Diaz"'
Autor:
Jorge D. Brioni, Tracy L. Carr, Gin C. Hsieh, Madhavi Pai, Lawrence A. Black, Tiffany Runyan Garrison, Cenchen Zhan, Marlon D. Cowart, Erica Gomez, Gilbert Diaz, Arlene M. Manelli, Marina I. Strakhova, Anthony Lee, Jill M. Wetter
Publikováno v:
European Journal of Pharmacology. 684:87-94
Histamine H(3) receptor antagonists have been widely reported to improve performance in preclinical models of cognition, but more recently efficacy in pain models has also been described. Here, A-960656 ((R)-2-(2-(3-(piperidin-1-yl)pyrrolidin-1-yl)be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::54c0e87b77f27eefbbaad46501b1babe
https://doi.org/10.1016/j.ejphar.2012.03.048
https://doi.org/10.1016/j.ejphar.2012.03.048
Characterization of A-935142, a hERG enhancer, in the presence and absence of standard hERG blockers
Autor:
Bryan F. Cox, Xiaoqin Liu, Gary A. Gintant, James T. Limberis, Gilbert Diaz, Ruth L. Martin, Kathryn Houseman, Zhi Su
Publikováno v:
Life Sciences. 90:607-611
Aims In a previous study we found that A-935142 enhanced hERG current in a concentration-dependent manner by facilitating activation, reducing inactivation, and slowing deactivation (Su et al., 2009). A-935142 also shortened action potential duration
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef24215cc71f2aa845920e90e5983a84
https://doi.org/10.1016/j.lfs.2012.02.017
https://doi.org/10.1016/j.lfs.2012.02.017
Autor:
Peter F. Bousquet, Daniel H. Albert, Gary A. Gintant, Patrick A. Marcotte, Gilbert Diaz, George A. Cunha, Ruth L. Martin, Kathryn Houseman, Stevan W. Djuric, Jürgen Dinges, Jennifer J. Bouska, Thomas J. Sowin, Paul Tapang, Charles W. Hutchins, Michael R. Michaelides, Kimba L. Ashworth, Eric F. Johnson, Henry Q. Zhang, Irini Akritopoulou-Zanze, Michelle Nyein, Arnold Lee D, Hu Li, Steven K. Davidsen, Alan F. Gasiecki, Christopher M. Harris, Vijaya Gracias, Zhi Su, Zhiren Xia
Publikováno v:
Journal of Medicinal Chemistry. 50:2011-2029
The synthesis of a novel series of 1,4-dihydroindeno[1,2-c]pyrazoles with acetylene-type side chains is described. Optimization of those compounds as KDR kinase inhibitors identified 8, which displayed an oral activity in an estradiol-induced murine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa7224e585fce7d1645dd21a1f5e3e55
https://doi.org/10.1021/jm061223o
https://doi.org/10.1021/jm061223o
Autor:
Ivan Milicic, Jorge D. Brioni, Deliang Zhou, Gerard B. Fox, Gerard D. Gagne, Ramin Faghih, Angela L. Molesky, Arthur A. Hancock, Kennan C. Marsh, Liping Pan, David G. Witte, Timothy A. Esbenshade, Jill M. Wetter, Kaitlin E. Browman, Michael J. Buckley, Gilbert Diaz, Xiaoqing Deng, Victoria A. Komater, John L. Baranowski, Thomas R. Miller, Marlon D. Cowart, Gregory A. Gfesser, Marilyn S. Diehl, Kathleen M. Krueger, Ellen M. Roberts
Publikováno v:
Biochemical Pharmacology. 73:1243-1255
Three novel heterocyclic benzofurans A-688057 ( 1 ), A-687136 ( 2 ), and A-698418 ( 3 ) were profiled for their in vitro and in vivo properties as a new series of histamine H 3 receptor antagonists. The compounds were all found to have nanomolar pote
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2fc1120f3945a2a50635d43ffdb23648
https://doi.org/10.1016/j.bcp.2007.02.010
https://doi.org/10.1016/j.bcp.2007.02.010
Autor:
Gilbert Diaz, Lee C. Preusser, Ann Mikhail, Christopher A. Ogiela, Lynch John K, Philip R. Kym, Lisa M. Hernández, Dariusz Wodka, Gang Zhao, Doug H. Falls, Eugene N. Bush, James S. Polakowski, Andrew S. Judd, Robin Shapiro, Hing L. Sham, James J. Napier, Christine A. Collins, Kennan C. Marsh, Victoria Knourek-Segel, Glenn A. Reinhart, Thomas J Campbell, Sevan Brodjian, Michael E. Brune, Brian A. Droz, Mathew M. Mulhern, Kathryn Houseman, Regina M. Reilly, Brian D. Dayton, Ryan M. Fryer, James T. Limberis, Rajesh R. Iyengar, Freeman Jennifer C
Publikováno v:
Journal of Medicinal Chemistry. 49:6569-6584
Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascualar assay led to the identification of a chromone-2-carboxamide series as having excellent safety against t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b667ab564d57ac2f27112dd9382a72ab
https://doi.org/10.1021/jm060683e
https://doi.org/10.1021/jm060683e
Autor:
Daryl R. Sauer, Jonathan Greer, Charles J. Nichols, Craig D. Wegner, Jason A. Segreti, Kurt M. Mohning, Fortuna Haviv, John T. Randolph, E N Bush, Philip L. Waid, Gilbert Diaz, Leslie M. Besecke, Gary Bammert
Publikováno v:
Journal of Medicinal Chemistry. 47:1085-1097
The design and synthesis of a series of 11,12-cyclic carbamate derivatives of 6-O-methylerythromycin A that are novel, nonpeptide LHRH antagonists, is described. The macrolide antagonist 1, discovered during a screen of our chemical repository, was c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3fabef2f09ac213c5e8373f774e466e4
https://doi.org/10.1021/jm030418i
https://doi.org/10.1021/jm030418i
Autor:
James S. Polakowski, Nathan L. Lubbers, Sandra E. Burke, Katina M Daniell, Bryan F. Cox, Craig D. Wegner, Gilbert Diaz
Publikováno v:
European Journal of Pharmacology. 435:79-83
Bimoclomol has been shown to increase an inducible member of the heat shock protein 70 family (HSP70) and cytoprotect in vitro. Here, we addressed whether oral pretreatment of rats with bimoclomol could elevate myocardial HSP70 and reduce infarct siz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7b78ac2bcba8f49cc9f88e5bf2b58b4
https://doi.org/10.1016/s0014-2999(01)01552-7
https://doi.org/10.1016/s0014-2999(01)01552-7
Autor:
Kurt M. Mohning, E N Bush, Van A. Cybulski, Craig D. Wegner, Gilbert Diaz, Randolph John, Mira Rao, Jason A. Segreti, Jonathan Greer, Fortuna Haviv, Philip L. Waid, Leslie M. Besecke
Publikováno v:
Drug Development Research. 52:485-491
Gonadotropin-releasing hormone (GnRH) stimulates the synthesis and secretion of the gonadotropins that maintain the reproductive axis in mammals. Efforts have focused on the characterization of novel, nonpeptidic orally active antagonists of the GnRH
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::34863a63a9805da58bf9feed4e71ffc9
https://doi.org/10.1002/ddr.1150
https://doi.org/10.1002/ddr.1150
Autor:
Marlon, Cowart, Gin, Hsieh, Lawrence A, Black, Cenchen, Zhan, Erica J, Gomez, Madhavi, Pai, Marina, Strakhova, Arlene, Manelli, Tracy, Carr, Jill, Wetter, Anthony, Lee, Gilbert, Diaz, Tiffany, Garrison, Jorge D, Brioni
Publikováno v:
European journal of pharmacology. 684(1-3)
Histamine H(3) receptor antagonists have been widely reported to improve performance in preclinical models of cognition, but more recently efficacy in pain models has also been described. Here, A-960656 ((R)-2-(2-(3-(piperidin-1-yl)pyrrolidin-1-yl)be
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::764e1b80d58c593fcd9bbd7cfee9c6b9
https://pubmed.ncbi.nlm.nih.gov/22504024
https://pubmed.ncbi.nlm.nih.gov/22504024
Autor:
Ruth L. Martin, Lee C. Preusser, James T. Limberis, Michael Meyer, Michael J. Dart, Betty B. Yao, Jonathon Green, Xiaoqin Liu, Gary A. Gintant, Zhi Su, Bryan F. Cox, James S. Polakowski, Gilbert Diaz
Publikováno v:
Current drug safety. 6(5)
A-955840, a selective CB2 agonist, has been shown to elicit concentration-dependent decreases in cardiac contractility in the anesthetized dog (decreased maximal velocity of left ventricular pressure development [LV dP/dt max]). However, it is unknow
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af8945b9999e6d964885523337f00520
https://pubmed.ncbi.nlm.nih.gov/22424534
https://pubmed.ncbi.nlm.nih.gov/22424534