Zobrazeno 1 - 10
of 13
pro vyhledávání: '"David James Hallett"'
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:
Gerard R. Dawson, David S. Reynolds, Elizabeth M. Garrett, Sharlene Bull, Paul J. Whiting, John R. Atack, Richard J. Newman, Thomas W. Rosahl, Rosa L. Fradley, Gillian F. O'Meara, Simon Charles Goodacre, Keith A. Wafford, David James Hallett, Martin R. Guscott
Publikováno v:
Journal of Psychopharmacology. 21:384-391
Non-selective benzodiazepines, such as diazepam, interact with equivalent affinity and agonist efficacy at GABAA receptors containing either an α1, α2, α3 or α5 subunit. However, which of these particular subtypes are responsible for the anticonv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eeb1c1f5ea624866cd6383cf6437e3e2
https://doi.org/10.1177/0269881106067255
https://doi.org/10.1177/0269881106067255
Autor:
Martin R. Guscott, Amy Davies, David S. Reynolds, James O. Groves, Keith A. Wafford, Thomas W. Rosahl, David James Hallett, Andrew Pike
Publikováno v:
European Journal of Neuroscience. 24:167-174
The majority of inhibitory neurotransmission in the brain is mediated by the gamma-aminobutyric acid (GABA) type A (GABA(A)) receptor. The anticonvulsant loreclezole largely acts by potentiating GABA(A) receptors containing beta2 and beta3 subunits.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09ead0facef45a22db407a52a2a54029
https://doi.org/10.1111/j.1460-9568.2006.04890.x
https://doi.org/10.1111/j.1460-9568.2006.04890.x
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3256a1392c1eb18c5f05fe4684c424b7
https://doi.org/10.1021/jm051144x
https://doi.org/10.1021/jm051144x
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab2e3f49e1fb5468f2d9ea9405f453b8
https://doi.org/10.1016/j.bmcl.2005.12.044
https://doi.org/10.1016/j.bmcl.2005.12.044
Autor:
Kevin John Merchant, Steve Thomas, Emanuela Gancia, Alexander Charles Humphries, David James Hallett, Myra Gilligan, Simon Charles Goodacre
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1518-1522
8-Fluoroimidazo[1,2-a]pyridine has been established as a physicochemical mimic of imidazo[1,2-a]pyrimidine, using both in silico and traditional techniques. Furthermore, a novel synthesis of a 3,7-disubstituted-8-fluoroimidazopyridine 3 has been deve
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef699f532ab3641ad2926a675b84cab8
https://doi.org/10.1016/j.bmcl.2005.12.037
https://doi.org/10.1016/j.bmcl.2005.12.037
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:
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3b0dd96fcc598d89a504d83e49c338d
https://doi.org/10.1021/jm051065l
https://doi.org/10.1021/jm051065l
Autor:
Simon Charles Goodacre, Michael Rowley, Ute Gerhard, Laure Hitzel, Steven R. Thomas, Richard G. Ball, Timothy Jason Sparey, David James Hallett
Publikováno v:
The Journal of Organic Chemistry. 65:4984-4993
A rearrangement reaction involving the indole nucleus was investigated using stereochemical markers and low-temperature NMR experiments. Treatment of (3S, 4S)-3-hydroxy-4-(2-phenyl-1H-indol-3-yl)-piperidine-1-carboxylic acid benzyl ester (90% ee) wit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ebd420d13d5e12e306a4a80b62ad834
https://doi.org/10.1021/jo0004759
https://doi.org/10.1021/jo0004759
Autor:
Mark J. Gemkow, Timothy D. Jones, David James Hallett, Christopher Charles Stimson, Adam James Davenport, Darshan G. Vaidya, Massimo Corsi, Edward Glenn, Sarah K. Bailey, Ulrike Fritz
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(17)
A series of potent and subtype selective H3 receptor antagonists containing a novel tetrazole core and diamine motif is reported. A one-pot multi-component Ugi reaction was utilised to rapidly develop the structure–activity relationships (SAR) of t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9060bcb1bde54fce0b175ea367e26543
https://pubmed.ncbi.nlm.nih.gov/20667729
https://pubmed.ncbi.nlm.nih.gov/20667729