Zobrazeno 1 - 10
of 57
pro vyhledávání: '"George R. Marshall"'
Autor:
Susanne G. Warner, Horacio J. Asbun, An-Lin Cheng, Alexandra M. Roch, George R. Marshall, Adnan Alseidi, Zeljka Jutric, Jan Grendar, Farzad Alemi, Paul D. Hansen, Elliot J. Scott, Eugene P. Ceppa, L.L. Pereira
Publikováno v:
HPB. 22:1216-1221
Background Optimal treatment of pancreatic ductal adenocarcinoma of the neck, body and tail (PDAC-NBT) necessitates R0 surgical resection. Preoperative radiographic identification of patients likely to achieve successful oncologic resection remains d
Autor:
Wayne F. A. Sheppard, David S. Reynolds, Alison J. Smith, John R. Atack, Joanna Stanley, David James Hallett, Richard Thomas Lewis, Keith A. Wafford, Rowan A. Wilson, Timothy Blackburn, George R. Marshall, Wesley Peter Blackaby, Andrew Pike, Spencer J. Tye, Andrew Stephen Robert Jennings, Susan M. Cook, Pushpinder Ferris, Bindi Sohal
Publikováno v:
Journal of Medicinal Chemistry. 49:2600-2610
The development of a series of GABA(A) alpha2/alpha3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably alpha3-selectiv
Autor:
George R. Marshall, Rachael Lincoln, Richard Thomas Lewis, Bindi Sohal, Susan M. Cook, Keith A. Wafford, John R. Atack, David James Hallett, Alison J. Smith, David S. Reynolds, Spencer J. Tye, Leslie J. Street, Michael G. N. Russell, Andrew Stephen Robert Jennings, Andrew Pike, José L. Castro, Joanna Stanley, Wayne F. A. Sheppard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1477-1480
Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABA(A) receptors that are functionally selective for the alpha2/alpha3 subtypes over the alpha1 subtype. SAR studies to optimise this fun
Autor:
Wesley Peter Blackaby, George R. Marshall, Richard Thomas Lewis, Simon Charles Goodacre, John R. Atack, David James Hallett, Leslie J. Street, Frances A. Bromidge, Andrew Pike, Alison J. Smith, David F. Tattersall, Keith A. Wafford, José L. Castro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1175-1179
Imidazo[1,2-a]pyrimidines are GABA(A) receptor benzodiazepine binding site ligands which can exhibit functional selectivity for the alpha(3) subtype over the alpha(1) subtype. SAR studies to optimize this functional selectivity are described.
Autor:
Wesley Peter Blackaby, Susan M. Cook, Alison J. Smith, Sarah Kelly, N. Brown, John R. Atack, Pushpinder Ferris, José L. Castro, Simon Charles Goodacre, Bindi Sohal, James Michael Crawforth, Joanna Stanley, Keith A. Wafford, David James Hallett, Andrew Pike, Richard Thomas Lewis, Leslie J. Street, George R. Marshall, Andrew Pate Owens
Publikováno v:
Journal of Medicinal Chemistry. 49:35-38
A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimid
Autor:
Jeremy J. Lambert, Keith A. Wafford, Signe í Stórustovu, Cecilia M. Borghese, Bjarke Ebert, Delia Belelli, R. Adron Harris, George R. Marshall, Murray B. Herd
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 316:1360-1368
GABA(A) receptors (GABA(A)Rs) are usually formed by alpha, beta, and gamma or delta subunits. Recently, delta-containing GABA(A)Rs expressed in Xenopus oocytes were found to be sensitive to low concentrations of ethanol (1-3 mM). Our objective was to
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
Autor:
Peter H. Hutson, Susan M. Cook, Gerard R. Dawson, John R. Atack, Ian Collins, Christopher Moyes, Keith A. Wafford, Graham D Bentley, George R. Marshall, Ruth M. McKernan, Neil Collinson
Publikováno v:
British Journal of Pharmacology. 144:357-366
Alpha3IA (6-(4-pyridyl)-5-(4-methoxyphenyl)-3-carbomethoxy-1-methyl-1H-pyridin-2-one) is a pyridone with higher binding and functional affinity and greater inverse agonist efficacy for GABA(A) receptors containing an alpha3 rather than an alpha1, alp
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
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.