Zobrazeno 1 - 10 of 62 pro vyhledávání: '"F. Emms"'
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4
1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1,3-dihydroimidazol-2-one: A Selective High-Affinity Antagonist for the Human Dopamine D4 Receptor with Excellent Selectivity over Ion Channels
Autor: Kevin W. Moore, Robert W. Carling, F. Emms, Bindi Sohal, Paul D. Leeson, Smita Patel, R. Marwood, Elizabeth A. Jones, Margaret S. Beer, Christopher Moyes, Shil Patel, Alan E. Fletcher, Katrine Bonner, and Andrew Pike
Publikováno v: Journal of Medicinal Chemistry. 42:2706-2715
After the requirement of pseudocycle formation in the ureas 3 and 7 for hD(4) binding and selectivity was confirmed, structural hybridization with the known hD(4) ligand 2 led to the design and identification of the lead 4-(2-oxo-1, 3-dihydroimidazol
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abf62362c8530ef5379105e9ec0ff09e
https://doi.org/10.1021/jm991029k
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5
4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors
Autor: Robert W. Carling, Elizabeth A. Jones, F. Emms, Shil Patel, Steven R. Thomas, Kevin W. Moore, Katrine Bonner, R. Marwood, Michael Rowley, Smita Patel, Paul D. Leeson
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:1285-1290
The syntheses of a number of different N-linked heterocyclic pyrazole replacements based on the structure 1 are described (compounds 3-12) as hD4 ligands. After further optimisation the best compound identified was 13 which has high affinity for hD4
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d5a3d1bec0264365b6a1e09f449f69f
https://doi.org/10.1016/s0960-894x(99)00169-9
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6
Regional Differences in the Inhibition of Mouse In Vivo [3H]Ro 15-1788 Binding Reflect Selectivity for α1 versus α2 and α3 Subunit-Containing GABAA Receptors
Autor: Alison J. Smith, F. Emms, Ruth M. McKernan, John R. Atack
Publikováno v: Neuropsychopharmacology. 20:255-262
The benzodiazepines flunitrazepam, diazepam, and Ro 15-1788 and the beta-carboline DMCM bind with equivalent affinity to the benzodiazepine binding site of GABAA receptors containing different alpha subunits (i.e., alpha 1, alpha 2, alpha 3, or alpha
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd2f3d2b640679d5478a6848d0fd572b
https://doi.org/10.1016/s0893-133x(98)00052-9
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7
Photoaffinity Labeling of the Benzodiazepine Binding Site of α1β3γ2 γ-Aminobutyric AcidAReceptors with Flunitrazepam Identifies a Subset of Ligands that Interact Directly with His102 of the α Subunit and Predicts Orientation of These within the Benzodiazepine Pharmacophore
Autor: Ian Collins, F. Emms, Sophie J. Farrar, Ruth M. McKernan, K Quirk, Howard B. Broughton, Ayodeji Asuni
Publikováno v: Molecular Pharmacology. 54:33-43
Photoincorporation of ligands into the benzodiazepine site of native gamma-aminobutyric acidA (GABAA) receptors provides useful information about the nature of the benzodiazepine (BZ) binding site. Photoincorporation of flunitrazepam into a single po
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b875b85e0c08ab405ca74347d12f482d
https://doi.org/10.1124/mol.54.1.33
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8
4-Heterocyclyl tetrahydropyridines as selective ligands for the human dopamine D4 receptor
Autor: Janusz Josef Kulagowski, R. Marwood, F. Emms, T. Harrison, Mark Peter Ridgill, Paul D. Leeson, Karen Elizabeth Haworth, Martin Richard Teall, K.L. Moss, M. Fielding, Kerry L. Chapman, S. Patel, Andrew Pate Owens
Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:2211-2216
A series of 1,2,3,6-tetrahydropyridines 3 were synthesised, which resulted in selective high affinity dopamine D4 ligands. The SAR of heterocyclic replacements and aromatic substitution was investigated, leading to compounds of nanomolar binding affi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::52e8b91c1ebe874bd4d881fcae977b1d
https://doi.org/10.1016/s0960-894x(97)00402-2
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10
Synthesis and sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands
Autor: F. Emms, Smita Patel, Neil Roy Curtis, Mark Peter Ridgill, Stephen B. Freedman, Paul D. Leeson, Janusz Jozef Kulagowski, Shil Patel
Publikováno v: Bioorganicmedicinal chemistry letters. 9(4)
7-azaindole compounds bearing a cyclic amine moiety linked by a one or two carbon chain attached at the 2- or 3-position were synthesised and evaluated as potential dopamine D4 ligands. Highest affinity and selectivity for the D4 receptor resided in
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3eecac56bbc464add15c404813a0ad4
https://pubmed.ncbi.nlm.nih.gov/10098669
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