Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Wai-Si Eng"'
Autor:
Hong Fan, Georgia B. McGaughey, Izzat T. Raheem, Mona Purcell, Liza Gantert, Marie A. Holahan, Youwei Yan, Sean M. Smith, Kerry Riffel, Xiangjun Meng, Paul J. Coleman, Jeffrey L. Evelhoch, Wai-Si Eng, Eric D. Hostetler, Aniket Joshi, Christopher D. Cox, John J. Renger, Broc A. Flores
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4893-4898
Phosphodiesterase 10A (PDE10A) inhibition has recently been identified as a potential mechanism to treat multiple symptoms that manifest in schizophrenia. In order to facilitate preclinical development and support key proof-of-concept clinical trials
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::25771a4490bc96538346e9692b6a3f4b
https://doi.org/10.1016/j.bmcl.2015.05.080
https://doi.org/10.1016/j.bmcl.2015.05.080
Autor:
Atack, John R.1 JAtack1@its.jnj.com, Wai-si Eng2, Gibson, Ray E.2, Ryan, Christine2, Francis, Barbara2, Sohal, Bindi1, Dawson, Gerard R.1, Hargreaves, Richard J.2, Burns, H. Donald2, Eng, Wai-Si (AUTHOR)
Publikováno v:
British Journal of Pharmacology. Jul2009, Vol. 157 Issue 5, p796-803. 8p. 2 Charts, 5 Graphs.
Autor:
David Wilson, Bindhu V. Karanam, Mona Purcell, Maria Madeira, Gary G. Chicchi, Jianming Bao, Liza Gantert, Robert J. DeVita, Huagang Lu, Wai-Si Eng, Sander G. Mills, Richard G. Ball, Andrew J. Kassick, Peter Lin, Sanjeev Kumar, Jaime Lynn Bunda, George A. Doss, Kwei-Lan C. Tsao, Jacquelyn J. Cook, Xinchun Tong, Richard Tschirret-Guth, Jinlong Jiang, Koppara Samuel, Richard Hargreaves, Hong Wang, Donald F. Hora
Publikováno v:
Journal of Medicinal Chemistry. 56:5940-5948
Hydroisoindoline 2 has been previously identified as a potent, brain-penetrant NK1 receptor antagonist with a long duration of action and improved profile of CYP3A4 inhibition and induction compared to aprepitant. However, compound 2 is predicted, ba
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::94febe29ddadade1fbafbe0e7e0c71d3
https://doi.org/10.1021/jm400751p
https://doi.org/10.1021/jm400751p
Autor:
Hisashi Ohta, Sandra M. Sanabria-Bohórquez, Michael F. Egan, Satoshi Ozaki, Guy Bormans, Kerry Riffel, William Cho, Marleen Depré, Shailendra Patel, Wai-Si Eng, Jacquelynn J. Cook, Tom Reynders, Raymond E. Gibson, Stephen Krause, Koen Van Laere, Christine Ryan, Sheng Bi, Stacey O'Malley, Osamu Okamoto, Eric D. Hostetler, Richard Hargreaves, Hiroshi Kawamoto, Aniket Joshi, Inge De Lepeleire, Tjibbe de Groot, H. Donald Burns, Jan de Hoon
Publikováno v:
NeuroImage. 68:1-10
Antagonism of the central opioid receptor like-1 receptor (ORL1) has been implicated in cognition, and has been a focus of drug discovery efforts to ameliorate the cognitive deficits that remain during the stable treatment of schizophrenia with curre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::75efc34d85dc68330a38fb08b31a4f83
https://doi.org/10.1016/j.neuroimage.2012.11.053
https://doi.org/10.1016/j.neuroimage.2012.11.053
Autor:
Hisashi Ohta, Satoru Ito, Christine Ryan, Gentaroh Suzuki, Jacquelynn J. Cook, Shil Patel, Mangay Williams, Satoshi Ozaki, Stephen Krause, Kerry Riffel, Eric D. Hostetler, Richard Hargreaves, Wai-Si Eng, Stacey O'Malley, Hiroshi Kawamoto, Aniket Joshi, H. Donald Burns, Sandra M. Sanabria-Bohórquez
Publikováno v:
Synapse. 65:125-135
Two moderately lipophilic, high affinity ligands for metabotropic glutamate receptor subtype 1 (mGluR1) were radiolabeled with a positron-emitting radioisotope and evaluated in rhesus monkey as potential PET tracers. Both ligands were radiolabeled wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a7c27020ffdfb172d5ff55f79a24c624
https://doi.org/10.1002/syn.20826
https://doi.org/10.1002/syn.20826
Autor:
Wai‐Si Eng, Glenn D. Prestwich
Publikováno v:
Bulletin des Sociétés Chimiques Belges. 95:895-914
Radiolabeled juvenile hormone (JHs) and labeled JH derivatives are required for the study of JH metabolism and JH-protein interactions as well as JH radioimmunoassay in insects. The progress in the synthesis of these labeled compounds for the last fi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::71cbfc6b3362f98f0baf58f502b07c93
https://doi.org/10.1002/bscb.19860950913
https://doi.org/10.1002/bscb.19860950913
Autor:
Sandra M. Sanabria-Bohórquez, J. N. de Hoon, K. Van Laere, Richard Hargreaves, Raymond E. Gibson, Spencer J. Tye, Leslie J. Street, Ruth M. McKernan, I De Lepeleire, Robert W. Carling, Keith A. Wafford, Andrew Pike, John R. Atack, Guy Bormans, Christine Ryan, David James Hallett, HD Burns, M. G Murphy, Wai-Si Eng, A. Van Hecken, G. R. Dawson
Publikováno v:
Journal of Psychopharmacology. 25:329-344
In the accompanying paper we describe how MRK-409 unexpectedly produced sedation in man at relatively low levels of GABAA receptor occupancy (∼10%). Since it was not clear whether this sedation was mediated via the α2/α3 or α1 GABAA subtype(s),
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ea0a5ae22a6d2851dd26b1e9a8bbbb4
https://doi.org/10.1177/0269881109354928
https://doi.org/10.1177/0269881109354928
Autor:
Sandra Sanabria, Laura Vessy, H. Donald Burns, Jean-Claude Baron, Richard Hargreaves, Michael L. Schrag, José M. Vega, Robert F. Dannals, Raymond E. Gibson, John S. Beech, Dean F. Wong, John R. Atack, Wai Si Eng, Ruth M. McKernan, Franklin I. Aigbirhio, Tim D. Fryer, Paul Scott-Stevens, Bindi Sohal, Christine Ryan, Yun Zhou
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 332:17-25
The GABA(A) receptor alpha2/alpha3 subtype-selective compound 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023; also known as MK-0777) is a triazolopyridazine that has similar,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f325d96a51632434ec234c4602261192
https://doi.org/10.1124/jpet.109.157909
https://doi.org/10.1124/jpet.109.157909
Autor:
Ray E Gibson, Gerard R. Dawson, Wai-Si Eng, H. Donald Burns, Barbara Francis, Christine Ryan, Bindi Sohal, John R. Atack, Richard Hargreaves
Publikováno v:
British Journal of Pharmacology. 157:796-803
alpha5IA (3-(5-methylisoxazol-3-yl)-6-[(1-methyl-1,2,3-triazol-4-yl)methyloxy]-1,2,4-triazolo[3,4-a]phthalazine) is a triazolophthalazine with subnanomolar affinity for alpha1-, alpha2-, alpha3- and alpha5-containing GABA(A) receptors. Here we have e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f01a4e71e3a806d31c6369513baff3e
https://doi.org/10.1111/j.1476-5381.2009.00216.x
https://doi.org/10.1111/j.1476-5381.2009.00216.x
Autor:
Wai-Si Eng, Xinchun Tong, Richard Tschirret-Guth, Song Zheng, Gary G. Chicchi, Geoge A. Doss, Koppara Samuel, Richard Hargreaves, Terence G. Hamill, Marc M. Kurtz, Robert J. DeVita, Sanjeev Kumar, Alan Wheeldon, Emma J. Carlson, Alana Upthagrove, Jaime Lynn Bunda, Stephen Krause, Jinlong Jiang, Christine Ryan, Sander G. Mills, Donald Burns, Kwei-Lan C. Tsao
Publikováno v:
Journal of Medicinal Chemistry. 52:3039-3046
3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one (17) is a high affinity, brain-penetrant, hydroisoindoline-based neurokinin-1 (NK(1)) receptor antagonist with a lo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d21762545018b32ec2dc16a2b6444d66
https://doi.org/10.1021/jm8016514
https://doi.org/10.1021/jm8016514