Zobrazeno 1 - 10
of 50
pro vyhledávání: '"Margaret S. Beer"'
Autor:
Jamil I. Bacha, George McAllister, Heather A. Skynner, Tim Bonnert, Paul C. Guest, Kamran Salim, Julie Kerby, Hector Urien-Rodriguez, Margaret S. Beer, Anne Heald, Tim R. Fenton, Emma Watts
Publikováno v:
Journal of Biological Chemistry. 277:15482-15485
Recent studies have shown that G-protein-coupled receptors (GPCRs) can assemble as high molecular weight homo- and hetero-oligomeric complexes. This can result in altered receptor-ligand binding, signaling, or intracellular trafficking. We have co-tr
Autor:
Margaret S. Beer, Linda J. Bristow, George McAllister, Howard B. Broughton, M.R. Knowles, Robert J. Baker, Michael G. N. Russell, José L. Castro, Laura Barden, Smita Patel
Publikováno v:
Journal of Medicinal Chemistry. 44:3881-3895
A series of N(1)-arylsulfonyltryptamines were found to be potent ligands of the human serotonin 5-HT(6) receptor with the 5-methoxy-1-benzenesulfonyl analogue (19) having the highest affinity. Additionally, it was discovered that a group such as 3-(3
Autor:
Pengilley Rr, Bindi Sohal, Victor G. Matassa, van Niel Mb, Josephine A. Stanton, Howard B. Broughton, Michael G. N. Russell, A. P. Watt, Margaret S. Beer, Castro Jl, Laure Hitzel
Publikováno v:
Journal of Medicinal Chemistry. 42:4981-5001
Several 5-HT(1D/1B) receptor agonists are now entering the marketplace as treatments for migraine. This paper describes the development of selective h5-HT(1D) receptor agonists as potential antimigraine agents which may produce fewer side effects. A
Autor:
Alan P. Watt, Angus Murray Macleod, Russell J. Mortishire-Smith, Margaret S. Beer, Peter W. Hunt, Desmond O'Connor, Castro Jl, Laure Hitzel, Monique Bodil Van Niel, Anne Heald, David C. Evans, Susan K. F. Cheng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:3243-3248
A solution phase synthesis for the preparation of 3-aryloxy-2-propanolamine libraries has been developed. This resulted in the identification of 5 as a ligand with dual affinity for 5-HT 1 A and serotonin re-uptake receptors which shows excellent pha
Autor:
Michael G. N. Russell, Josephine A. Stanton, Bindi Sohal, Russell J. Mortishire-Smith, Jose L. Castro, Margaret S. Beer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2491-2496
The conformational restriction of a (benzylamino)methyl substituted pyrrolidine to form 2,7-diazabicyclo[3.3.0]octanes has led to a series of compounds with high affinity at the h5-HT1D receptor as well as dramatically increased concentrations in the
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
Autor:
Ian Collins, M. B. Van Niel, Michael G. N. Russell, Michael Rowley, Karen L Locker, Desmond O'Connor, Denise Morrison, Susan Koon-Fung Cheng, Christopher Moyes, Josephine A. Stanton, Hugh M. Verrier, Simon Charles Goodacre, Anne Heald, Bindi Sohal, Andrew Pike, Angus Murray Macleod, Howard B. Broughton, Steve Thomas, Margaret S. Beer, Castro Jl, A. P. Watt
Publikováno v:
Journal of Medicinal Chemistry. 42:2087-2104
It has previously been reported that a 3-(3-(piperazin-1-yl)propyl)indole series of 5-HT1D receptor ligands have pharmacokinetic advantages over the corresponding 3-(3-(piperidin-1-yl)propyl)indole series and that the reduced pKa of the piperazines c
Autor:
Austin John Reeve, Josephine A. Stanton, Margaret S. Beer, Anne Heald, Leslie J. Street, Bindi Sohal, A. P. Watt, Alexander Richard Guiblin, Victor G. Matassa, Francine Sternfeld, Richard Alexander Jelley, Peter Alan Hunt
Publikováno v:
Journal of Medicinal Chemistry. 42:677-690
The design, synthesis, and biological evaluation of a novel series of 3-[2-(pyrrolidin-1-yl)ethyl]indoles with excellent selectivity for h5-HT1D (formerly 5-HT1Dalpha) receptors over h5-HT1B (formerly 5-HT1Dbeta) receptors are described. Clinically e
Autor:
Denise Rathbone, José L. Castro, Margaret S. Beer, Alan P. Watt, Josephine A. Stanton, Bindi Sohal, Ian Collins, Michael G. N. Russell
Publikováno v:
Journal of Medicinal Chemistry. 41:2667-2670
Autor:
Michael G. N. Russell, Josephine A. Stanton, Richard Alexander Jelley, Alexander Richard Guiblin, José L. Castro, Margaret S. Beer, Leslie J. Street, Francine Sternfeld, Victor G. Matassa
Publikováno v:
Journal of Medicinal Chemistry. 40:3497-3500