Zobrazeno 1 - 10
of 63
pro vyhledávání: '"Robert F, Bruns"'
Autor:
Stacy A. Castner, Linli Zhang, Charles R. Yang, Junliang Hao, Jeffrey W. Cramer, Xushan Wang, Robert F. Bruns, Hugh Marston, Kjell A. Svensson, Graham V. Williams
Publikováno v:
Psychopharmacology. 240:1033-1048
Rationale Dopamine (DA) signaling through the D1 receptor has been shown to be integral to multiple aspects of cognition, including the core process of working memory. The discovery of positive allosteric modulators (PAMs) of the D1 receptor has enab
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a6213ca6a6549d7eb6e405c83245911c
https://doi.org/10.1007/s00213-022-06282-7
https://doi.org/10.1007/s00213-022-06282-7
Autor:
Xushan Wang, Erik J. Hembre, Paul J. Goldsmith, James P. Beck, Kjell A. Svensson, Francis S. Willard, Robert F. Bruns
Publikováno v:
Molecular Pharmacology. 103:176-187
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7723d763402ad2f1fa7e81b92f95979a
https://doi.org/10.1124/molpharm.122.000605
https://doi.org/10.1124/molpharm.122.000605
Autor:
Robert F. Bruns, Qi Chen, Paloma Vidal, John Mehnert Schaus, Charles R. Yang, Stephen N. Mitchell, Steven Marc Massey, Nuria Diaz, Xushan Wang, David Andrew Coates, Rebecca A. Wright, Beverly A. Heinz, Kevin Matthew Gardinier, Greg Stephenson, James P. Beck, Rajni M. Bhardwaj, Julie F. Falcone, Bruce A. Dressman, Deanna L Maren, Anette M. Johansson, David Michael Remick, Jeff W. Cramer, Cohen Michael Philip, Brian Morgan Watson, Jeffery Richardson, Kjell Svensson, Xin Zhou, Erik James Hembre, Serge Louis Boulet, Reinhard Matthew Robert, Daniel S. Richards, Junliang Hao, David M. Bender, Guy Carter, Christopher David Beadle, Brian G. Getman, Wolfangel Craig Daniel, Diseroad Benjamin Alan, Jason K. Myers, Joseph H. Krushinski, David Edward Tupper
Publikováno v:
Journal of Medicinal Chemistry. 62:8711-8732
Clinical development of catechol-based orthosteric agonists of the dopamine D1 receptor has thus far been unsuccessful due to multiple challenges. To address these issues, we identified LY3154207 (...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5a353395d3c6f7ca6dfa78c95a347dd4
https://doi.org/10.1021/acs.jmedchem.9b01234
https://doi.org/10.1021/acs.jmedchem.9b01234
Autor:
Junliang, Hao, James P, Beck, John M, Schaus, Joseph H, Krushinski, Qi, Chen, Christopher D, Beadle, Paloma, Vidal, Matthew R, Reinhard, Bruce A, Dressman, Steven M, Massey, Serge L, Boulet, Michael P, Cohen, Brian M, Watson, David, Tupper, Kevin M, Gardinier, Jason, Myers, Anette M, Johansson, Jeffery, Richardson, Daniel S, Richards, Erik J, Hembre, David M, Remick, David A, Coates, Rajni M, Bhardwaj, Benjamin A, Diseroad, David, Bender, Greg, Stephenson, Craig D, Wolfangel, Nuria, Diaz, Brian G, Getman, Xu-Shan, Wang, Beverly A, Heinz, Jeff W, Cramer, Xin, Zhou, Deanna L, Maren, Julie F, Falcone, Rebecca A, Wright, Stephen N, Mitchell, Guy, Carter, Charles R, Yang, Robert F, Bruns, Kjell A, Svensson
Publikováno v:
Journal of medicinal chemistry. 62(19)
Clinical development of catechol-based orthosteric agonists of the dopamine D1 receptor has thus far been unsuccessful due to multiple challenges. To address these issues, we identified LY3154207 (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::38771cd6f379be26a1a0dc76826df19b
https://pubmed.ncbi.nlm.nih.gov/31532644
https://pubmed.ncbi.nlm.nih.gov/31532644
Publikováno v:
Advances in pharmacology (San Diego, Calif.). 86
The dopamine D1 receptor plays an important role in motor activity, reward, and cognition. Efforts to develop D1 agonists have been mixed due to poor drug-like properties, tachyphylaxis, and inverted U-shaped dose-response curves. Recently, positive
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::1c074c909524dfd6f897670086e7ffd9
https://pubmed.ncbi.nlm.nih.gov/31378255
https://pubmed.ncbi.nlm.nih.gov/31378255
The dopamine D1 receptor plays an important role in motor activity, reward, and cognition. Efforts to develop D1 agonists have been mixed due to poor drug-like properties, tachyphylaxis, and inverted U-shaped dose-response curves. Recently, positive
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bcdc2acbca8e70abd82250e3fc7bed8f
https://doi.org/10.1016/bs.apha.2019.06.001
https://doi.org/10.1016/bs.apha.2019.06.001
Autor:
Junliang Hao, Robert F. Bruns, Beverly A. Heinz, Joan H. Carter, James P. Beck, Kjell A. Svensson, Yue-Wei Qian, Sheila P. Little, Robert Alan Gadski, John Mehnert Schaus, Xushan Wang, Charles R. Yang, Lisa Selsam Beavers
Publikováno v:
Molecular pharmacology. 94(4)
The binding site for DETQ [2-(2,6-dichlorophenyl)-1-((1S,3R)-3-(hydroxymethyl)-5-(2-hydroxypropan-2-yl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one], a positive allosteric modulator (PAM) of the dopamine D1 receptor, was identified and compa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dfb145a6374970273781446aa5024dd7
https://pubmed.ncbi.nlm.nih.gov/30111649
https://pubmed.ncbi.nlm.nih.gov/30111649
Autor:
Michelle M Menezes, Jeffrey M. Witkin, Kjell A. Svensson, Brian J. Eastwood, Eyassu Chernet, Michael J. O'Neill, Julie F. Falcone, Keith A. Wafford, Hong Wang, Linda K. Thompson, John W. Ryder, Stephen N. Mitchell, Junliang Hao, John Mehnert Schaus, Robert F. Bruns, Alex J. Harper, Meghane E. Masquelin, Deanna L Maren, Xia Li, Tracey K. Murray, Charles R. Yang, Elaine Shanks, Jason Katner, Linli Zhang, Guy Carter, James P. Beck, Patrick L. Love
Publikováno v:
Neuropharmacology. 128
DETQ, an allosteric potentiator of the dopamine D1 receptor, was tested in therapeutic models that were known to respond to D1 agonists. Because of a species difference in affinity for DETQ, all rodent experiments used transgenic mice expressing the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4bdd0d92066c9741468043d0c8f34cb
https://pubmed.ncbi.nlm.nih.gov/29102759
https://pubmed.ncbi.nlm.nih.gov/29102759
Autor:
Junliang Hao, Wesley H. Anderson, Cohen Michael Philip, Kjell A. Svensson, Michael A. Statnick, Donald R. Gehlert, Joseph H. Krushinski, Hellman Sarah Lynne, Michelle M Menezes, Jeffrey W Cramer, Julie F. Falcone, Xushan Wang, Rebecca A. Wright, John Mehnert Schaus, Neil W. DeLapp, Reinhard Matthew Robert, S Michelle Morin, Charles R. Yang, Todd R. Wiernicki, Ilya Okun, Renee Emkey, Benjamin L. Adams, Beverly A. Heinz, Brian G. Getman, James P. Beck, Robert F. Bruns, Virginia L. Lucaites, Todd M. Suter, Deanna L Maren, David L. Nelson, Kelly L. Knopp, Borys V. Rogovoy
Publikováno v:
The Journal of Pharmacology and Experimental Therapeutics
Allosteric potentiators amplify the sensitivity of physiologic control circuits, a mode of action that could provide therapeutic advantages. This hypothesis was tested with the dopamine D1 receptor potentiator DETQ [2-(2,6-dichlorophenyl)-1-((1S,3R)-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::407266480ca7b482e7f8dd098b6484ac
https://pubmed.ncbi.nlm.nih.gov/27811173
https://pubmed.ncbi.nlm.nih.gov/27811173
Autor:
Jeffrey J. Skelton, Karine Fabio, Robin D. G. Cooper, Robert F. Bruns, Gary A. Koppel, Stephen W. Kaldor, David C. Hunden, Bruce A. Dressman, Michael P. Clay, Mitchell I. Steinberg, Michael J. Brownstein, Neal G. Simon, Christophe Guillon, Craig F. Ferris, Marvin J. Miller, Michael O. Chaney, Shi-fang Lu, Ned D. Heindel
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:2054-2080
The azetidinone LY307174 (1) was identified as a screening lead for the vasopressin V1a receptor (IC50 45 nM at the human V1a receptor) based on molecular similarity to ketoconazole (2), a known antagonist of the luteinizing hormone releasing hormone
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fcea47a4dc266c2aa7647f92ba4147e5
https://doi.org/10.1016/j.bmc.2006.12.031
https://doi.org/10.1016/j.bmc.2006.12.031