Zobrazeno 1 - 10
of 68
pro vyhledávání: '"Robert W. Carling"'
Autor:
Wenzheng Hu, Kangasmetsa Jussi J, Matthew Lawrence, C.S. Spada, Simon N. Pettit, David F. Woodward, Jose L. Martos, Jenny W. Wang, Neil J. Poloso, Robert W. Carling, L David Waterbury
Publikováno v:
ACS Pharmacol Transl Sci
[Image: see text] It has previously been reported that a prototypical compound (AGN 211377), which blocks pro-inflammatory prostanoid receptors (DP(1), DP(2), EP(1), EP(4,) FP, TP) and leaves open IP and EP(2) receptors so that their anti-inflammator
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa404d08d89bb58802fc3ffded7c5704
https://pubmed.ncbi.nlm.nih.gov/33344897
https://pubmed.ncbi.nlm.nih.gov/33344897
Autor:
David F. Woodward, Marco Allarà, Fabiana Piscitelli, Francesca Guida, Angela Amoresano, Jenny W. Wang, Livio Luongo, Rosa Maria Vitale, Cristoforo Silvestri, Vincenzo Di Marzo, Anna Illiano, Alessia Ligresti, Jose L. Martos, Pietro Amodeo, Gennaro Marino, Robert W. Carling, Sabatino Maione
Publikováno v:
ACS chemical neuroscience (2018). doi:10.1021/acschemneuro.8b00315
info:cnr-pdr/source/autori:Ligresti A.; Silvestri C.; Vitale R.M.; Martos J.L.; Piscitelli F.; Wang J.W.; Allara M.; Carling R.W.; Luongo L.; Guida F.; Illiano A.; Amoresano A.; Maione S.; Amodeo P.; Woodward D.F.; Di Marzo V.; Marino G./titolo:FAAH-Catalyzed C-C Bond Cleavage of a New Multitarget Analgesic Drug/doi:10.1021%2Facschemneuro.8b00315/rivista:ACS chemical neuroscience/anno:2018/pagina_da:/pagina_a:/intervallo_pagine:/volume
info:cnr-pdr/source/autori:Ligresti A.; Silvestri C.; Vitale R.M.; Martos J.L.; Piscitelli F.; Wang J.W.; Allara M.; Carling R.W.; Luongo L.; Guida F.; Illiano A.; Amoresano A.; Maione S.; Amodeo P.; Woodward D.F.; Di Marzo V.; Marino G./titolo:FAAH-Catalyzed C-C Bond Cleavage of a New Multitarget Analgesic Drug/doi:10.1021%2Facschemneuro.8b00315/rivista:ACS chemical neuroscience/anno:2018/pagina_da:/pagina_a:/intervallo_pagine:/volume
The discovery of extended catalytic versatilities is of great importance in both the chemistry and biotechnology fields. Fatty acid amide hydrolase (FAAH) belongs to the amidase signature superfamily and is a major endocannabinoid inactivating enzyme
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f3c3742f4f0d43e9590930ffd994e96
https://doi.org/10.1021/acschemneuro.8b00315
https://doi.org/10.1021/acschemneuro.8b00315
Autor:
Jenny Wang, David F. Woodward, Neil J. Poloso, Robert W. Carling, Ming Ni, Alex Bauer, Jose L. Martos
Publikováno v:
FASEB journal : official publication of the Federation of American Societies for Experimental Biology. 31(1)
The purpose of these studies was to test the hypothesis that a selected polypharmacological approach for treating the prostanoid-mediated component of inflammatory diseases would produce a therapeutic effect superior to global inhibition of prostagla
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bd48e720b31fad4d928d9eb8591a9f4
https://pubmed.ncbi.nlm.nih.gov/27770021
https://pubmed.ncbi.nlm.nih.gov/27770021
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:
Jason M, Elliott, Robert W, Carling, Gary G, Chicchi, James, Crawforth, Peter H, Hutson, A Brian, Jones, Sarah, Kelly, Rose, Marwood, Georgina, Meneses-Lorente, Elena, Mezzogori, Fraser, Murray, Michael, Rigby, Inmaculada, Royo, Michael G N, Russell, Duncan, Shaw, Bindi, Sohal, Kwei Lan, Tsao, Brian, Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5752-5756
Introduction of selected amine containing side chains into the 3-position of N',2-diphenylquinoline-4-carbohydrazide based NK3 antagonists abolishes unwanted hPXR activation. Introduction of a fluorine at the 8-position is necessary to minimize unwan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d704e07d074727d41f2d40a900255eb
https://doi.org/10.1016/j.bmcl.2006.08.085
https://doi.org/10.1016/j.bmcl.2006.08.085
Autor:
Robert W. Carling, Wesley Peter Blackaby, Andrew Mitchinson, Sylvie Bourrain, Richard Thomas Lewis
Publikováno v:
Tetrahedron Letters. 47:2257-2260
Novel syntheses of 2,3,8-trisubstituted pyrido[2,3- d ]pyridazines and 2,3,5-trisubstituted pyrazino[2,3- d ]pyridazines are described. Two complementary routes to pyrido[2,3- d ]pyridazines were developed, the first of which began by constructing th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::feaf8e32c8879e94ea5992207c5d8710
https://doi.org/10.1016/j.tetlet.2006.01.084
https://doi.org/10.1016/j.tetlet.2006.01.084
Autor:
Leslie J. Street, George R. Marshall, Bindi Sohal, Ruth M. McKernan, Andrew Mitchinson, Susan M. Cook, Andrew Pike, José L. Castro, Robert W. Carling, Timothy Harrison, Ian C. Ragan, Sally Ann Thompson, John R. Atack, K Quirk, Andrew Madin, Kevin W. Moore, Michael G. N. Russell, Alec Guiblin, Keith A. Wafford, Gerard R. Dawson, Pushpinder Ferris
Publikováno v:
Journal of Medicinal Chemistry. 48:7089-7092
There is increasing evidence that compounds with selectivity for gamma-aminobutyric acid(A) (GABA(A)) alpha2- and/or alpha3-subtypes may retain the desirable anxiolytic activity of nonselective benzodiazepines but possess an improved side effect prof
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5669d56878a0d056aa7267380a12e4df
https://doi.org/10.1021/jm058034a
https://doi.org/10.1021/jm058034a
Autor:
W. Rycroft, George R. Marshall, Neil Collinson, Mark Stuart Chambers, Angus Murray Macleod, Gerard R. Dawson, John R. Atack, Susan M. Cook, Desmond O'Connor, Sarah Christine Hobbs, Pushpindar Ferris, Robert W. Carling
Publikováno v:
Journal of Medicinal Chemistry. 47:5829-5832
(3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (13) has been identified as a functionally selective, inverse agonist at the benzodiazepine site of GABA(A) alpha5 receptors. 13 is orally
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66ee6f0a465b55f82b6f97720d100921
https://doi.org/10.1021/jm040863t
https://doi.org/10.1021/jm040863t
Autor:
Alison J. Smith, Leslie J. Street, Michael G. N. Russell, George R. Marshall, Robert W. Carling, Ruth M. McKernan, Kevin W. Moore, Andrew Mitchinson, Karen S. Curley, John R. Atack, Robert Narquizian, José L. Castro, Keith A. Wafford, Sally-Anne Thompson, Peter Blurton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:3441-3444
2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands with functional selectivity for the alpha3 subtype over the alpha1 subtype. SAR studies to optimise this functional selectivity are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20a0a030d4a5cc3ff2ccefb8cef252a7
https://doi.org/10.1016/j.bmcl.2004.04.085
https://doi.org/10.1016/j.bmcl.2004.04.085
Autor:
Sally A. Thompson, Leslie J. Street, Bindi Sohal, George R. Marshall, Susan M. Cook, Ruth M. McKernan, Guy R. Seabrook, Keith A. Wafford, Andrew Pike, John R. Atack, Gerard R. Dawson, Richard Alexander Jelley, Goplan V. Pillai, Francine Sternfeld, Kevin W. Moore, Frances A. Bromidge, José L. Castro, Angus Murray Macleod, Austin John Reeve, Robert W. Carling
Publikováno v:
Journal of Medicinal Chemistry. 47:3642-3657
The identification of a novel series of 7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines as GABA(A)alpha5 inverse agonists, which have both binding and functional (efficacy) selectivity for the benzodiazepine binding site of alpha5
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a33e28214a4b14c17e26fa56005fcc99
https://doi.org/10.1021/jm0407613
https://doi.org/10.1021/jm0407613