Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Frances A. Bromidge"'
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.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bac9dfff717bed7fe7f9f76e42c4294
https://doi.org/10.1016/j.bmcl.2005.11.112
https://doi.org/10.1016/j.bmcl.2005.11.112
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
Autor:
Paul J. Whiting, Frances A. Bromidge, Thomas W. Rosahl, David S. Reynolds, Robert J. Newman, John R. Atack, G. R. Dawson, Gillian F. O'Meara
Publikováno v:
Neuropharmacology. 44:190-198
The GABA(A) receptor system provides the major inhibitory control in the CNS, with the alpha 1 beta 2 gamma 2 subunit combination being the most abundant and widely distributed form of the receptor. The alpha1 subunit knock-out (alpha1 KO) mice had a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::61a56489c3aec247e418f4ae271fd539
https://doi.org/10.1016/s0028-3908(02)00370-2
https://doi.org/10.1016/s0028-3908(02)00370-2
Autor:
Paul J. Whiting, M. Anna Casula, Peter B. Wingrove, Frances A. Bromidge, Karen A. Maubach, Karine Martin, Guy R. Seabrook, K. L. Hadingham, Gopalan V. Pillai
Publikováno v:
Journal of Neurochemistry. 77:445-451
L-655,708 is a ligand for the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor that exhibits a 100-fold higher affinity for α5-containing receptors compared with α1-containing receptors. Molecular biology approaches have been
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e5ef9a56887f09ac75c9459e9ec8ec96
https://doi.org/10.1046/j.1471-4159.2001.00289.x
https://doi.org/10.1046/j.1471-4159.2001.00289.x
Autor:
Robert W. Carling, Elena Mezzogori, Spencer J. Tye, Rebecca Dias, Rachael Lincoln, Alison J. Smith, María Domínguez, Keith A. Wafford, Frances A. Bromidge, Simon Charles Goodacre, Susan M. Cook, Robert J. Newman, Andrew Pike, David James Hallett, Atack, Michael G. N. Russell, Wayne F. A. Sheppard, Pushpinder Ferris, Michael Reader, Leslie J. Street, George R. Marshall, Bindi Sohal, Joanna Stanley, Castro Jl, David S. Reynolds
Publikováno v:
Journal of medicinal chemistry. 49(4)
The identification of a series of imidazo[1,2-b][1,2,4]triazines with high affinity and functional selectivity for the GABA(A) alpha3-containing receptor subtype is described, leading to the identification of a clinical candidate, 11. Compound 11 sho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57692878f43ef6be13472e737d06c323
https://pubmed.ncbi.nlm.nih.gov/16480260
https://pubmed.ncbi.nlm.nih.gov/16480260
Autor:
Wesley Peter Blackaby, Frances A. Bromidge, Ruth M. McKernan, Michael G. N. Russell, Keith A. Wafford, John R. Atack, Alison J. Smith, Richard Thomas Lewis, Leslie J. Street, José L. Castro
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(22)
2,5-Dihydro-3H-pyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands, which can exhibit functional selectivity for the α3 subtype over the α1 subtype. SAR studies to optimize this functional selectivity are described.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fbe7534fdfd124abb03ee7112711769
https://pubmed.ncbi.nlm.nih.gov/16153832
https://pubmed.ncbi.nlm.nih.gov/16153832
Autor:
Robert W. Carling, Frances A. Bromidge, Catherine Isted, Alison J. Macaulay, José L. Castro, Peter W. Hunt, Ruth M. McKernan, Andrew Mitchinson, Matt Lucas, David W. Thomas, John R. Atack, Kevin W. Moore, Michael G. N. Russell, Keith A. Wafford, Susan M. Cook, Sally-Anne Thompson, Robert Narquizian
Publikováno v:
Journal of medicinal chemistry. 48(5)
We have previously identified the 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazine (1) as a potent partial agonist for the alpha(3) receptor subtype with 5-fold selectivity in binding affinity over alpha(1). This paper describes a det
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0c724106aa02b758bddd4fde74f7dc7
https://pubmed.ncbi.nlm.nih.gov/15743180
https://pubmed.ncbi.nlm.nih.gov/15743180
Autor:
Shil Patel, George McAllister, Josephine A. Stanton, Andrew Pate Owens, Paul J. Whiting, Martin R. Guscott, Kevin C. F. Fone, Stephany M. Biello, J Myers, Margaret S. Beer, K. L. Hadingham, Janusz Jozef Kulagowski, Frances A. Bromidge, Peter H. Hutson, Ian Thomas Huscroft, Thomas W. Rosahl, Nadia Melanie Rupniak, Linda J. Bristow
Publikováno v:
Neuropharmacology. 48(4)
The affinity of several antidepressant and antipsychotic drugs for the 5-HT7 receptor and its CNS distribution suggest potential in the treatment of psychiatric diseases. However, there is little direct evidence of receptor function in vivo to suppor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b5ce4c2820c481661443d18cc05cd26
https://pubmed.ncbi.nlm.nih.gov/15755477
https://pubmed.ncbi.nlm.nih.gov/15755477
Autor:
Ian Collins, John R. Atack, K Quirk, Bindi Sohal, Andrew Pike, Sally-Ann Thompson, Michael Rowley, Gerard R. Dawson, Richard G. Ball, José L. Castro, Christopher Moyes, William B Davey, Frances A. Bromidge, Keith A. Wafford, Nancy N. Tsou, Ruth M. McKernan
Publikováno v:
Journal of medicinal chemistry. 45(9)
A novel series of 3-heteroaryl-5,6-bis(aryl)-1-methyl-2-pyridones were developed with high affinity for the benzodiazepine (BZ) binding site of human gamma-aminobutyric acid (GABA(A)) receptor ion channels, low binding selectivity for alpha 2- and/or
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c69ddefbd8dce4e72545c5998e30f50
https://pubmed.ncbi.nlm.nih.gov/11960500
https://pubmed.ncbi.nlm.nih.gov/11960500
Autor:
Howard B. Broughton, Karen A. Maubach, Angus Murray Macleod, John R. Atack, Keith A. Wafford, Susan M. Cook, Mark Stuart Chambers, Gerard R. Dawson, Frances A. Bromidge, Guy R. Seabrook, Sarah Christine Hobbs, Austin John Reeve
Publikováno v:
Journal of medicinal chemistry. 45(6)
Nonselective inverse agonists at the benzodiazepine binding site on the GABA-A chloride ion channel enhance cognitive performance in animals but cannot be used in the treatment of cognitive disorders because of anxiogenic and convulsant side effects.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a00826f1d61e106c5080369f3b78070
https://pubmed.ncbi.nlm.nih.gov/11881985
https://pubmed.ncbi.nlm.nih.gov/11881985