Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Vicky Holland"'
Autor:
Neil Upton, Tania O. Stean, Claire Roberts, Michael S. Hadley, Vicky Holland, Gary W. Price, Laurie J. Gordon, Jeannette M. Watson, Jenifer Powles, Claire M. Scott, Leanne Cutler, Tanya Coleman, Tom D. Heightman, Andrew Ayrton, Jean-Pierre Pilleux, Sarah L. Pardoe, Graham J. Riley, Laramie Mary Gaster, Nigel E. Austin, Brenda K. Trail, Derek N. Middlemiss
The novel 8-piperazinyl-2,3-dihydropyrroloisoquinoline template was synthesized in nine steps. The template was N-substituted to give a series of compounds showing binding to human cloned 5-HT1A, 5-HT1B and 5-HT1D receptors with pKi’s greater than
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86421f00e16772e71fb543436a7895c9
https://doi.org/10.1016/j.bmcl.2005.06.042
https://doi.org/10.1016/j.bmcl.2005.06.042
Autor:
Kim Winborn, Sarah C. Lappin, James S. Wright, Vicky Holland, Martin J. Gunthorpe, Harshad Kantilal Rami, Andrew D. Randall, Sandra Arpino, Graham D Smith, Julie Egerton, Stephen J. Brough, Mervyn Thompson, Jeffrey C. Jerman, Sara Luis Hannan, Darren Smart, John B. Davis
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 321:1183-1192
Vanilloid receptor-1 (TRPV1) is a nonselective cation channel, predominantly expressed by sensory neurons, which plays a key role in the detection of noxious painful stimuli such as capsaicin, acid, and heat. TRPV1 antagonists may represent novel the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::519bdcb9b1541b2a29cae2ecf14a8d24
https://doi.org/10.1124/jpet.106.116657
https://doi.org/10.1124/jpet.106.116657
Autor:
Jenifer Powles, Neil Upton, Kim Winborn, Nigel Deeks, Christopher N. Johnson, Tania Buck, Mahmood Ahmed, Brenda K. Trail, Darren Jason Mitchell, Mervyn Thompson, Vicky Holland, Laurie J. Gordon, Michael A. Briggs, Jon T. Seal, Stephen Moss, Ashley Garner, David R. Witty, Steven Mark Bromidge, Lorraine Campbell, Andrew D. Medhurst, Tania O. Stean, Geoffrey Stemp, Dieter Hamprecht
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4867-4871
Starting from the potent and selective but poorly brain penetrant 5-HT6 receptor antagonist SB-271046, a successful strategy for improving brain penetration was adopted involving conformational constraint with concomitant reduction in hydrogen bond c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::235a4ea32a843eeea24f410f2584c393
https://doi.org/10.1016/j.bmcl.2005.06.107
https://doi.org/10.1016/j.bmcl.2005.06.107
Autor:
Neil Upton, Stephen J. Brough, Graham J. Riley, Kathryn R. Starr, Mark S. Duxon, Darren Smart, Jeff C. Jerman, Jennifer Stretton, Declan N.C. Jones, Vicky Holland, Roderick A. Porter, Amanda Johns, Wai Chan
Publikováno v:
Psychopharmacology. 153:203-209
Rationale: Orexins A and B have recently been discovered and shown to be derived from prepro-orexin, primarily expressed in the rat hypothalamus. Orexin-A has been ascribed a number of in vivo functions in the rat after intracerebroventricular (ICV)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fc21b93e05c58fb17a27f8b1e7989cf
https://doi.org/10.1007/s002130000550
https://doi.org/10.1007/s002130000550
Autor:
Vicky Holland, Frank King, Saunders Dv, Graham J. Riley, Thomas P. Blackburn, Derek N. Middlemiss, D.Malcolm Duckworth, Graham Elgin Jones, Jerome Jones, Steven Mark Bromidge, Sean Lightowler, Guy A. Kennett, Martyn D. Wood, Susannah Davies, Steven Dabbs, Ian Thomson Forbes, Brenda K. Trail
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:1863-1866
Bisaryl ethers have been identified with excellent 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 11, 27 and 38 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00d8da8ee47c7d42c8f4723c004ff055
https://doi.org/10.1016/s0960-894x(00)00364-4
https://doi.org/10.1016/s0960-894x(00)00364-4
Autor:
Ian Thomson Forbes, Peter Ham, Thomas P. Blackburn, Saunders Dv, Guy A. Kennett, Angela Gadre, D.Malcolm Duckworth, Vicky Holland, Martyn D. Wood, Deepa Vyas, Steven Dabbs, Graham J. Riley, David T. Davies, Frank King, Susannah Davies, Graham Elgin Jones, Steven Mark Bromidge, Kevin M. Thewlis
Publikováno v:
Bioorganic & Medicinal Chemistry. 7:2767-2773
A model series of 5-HT2C antagonists have been prepared by rapid parallel synthesis. These N-substituted phenyl-N'-pyridin-3-yl ureas were found to have a range of 5-HT2C receptor affinities and selectivities over the closely related 5-HT2A receptor.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::41e616c20825d452ab463c6f2fee997d
https://doi.org/10.1016/s0968-0896(99)00228-x
https://doi.org/10.1016/s0968-0896(99)00228-x
Autor:
Christopher B. Naylor, Vicky Holland, Susannah Starr, Kevin M. Thewlis, Martyn D. Wood, D.Malcolm Duckworth, Steven Mark Bromidge, Frank King, Thomas P. Blackburn, Steven Dabbs, Peter Ham, Saunders Dv, Graham Elgin Jones, Ian Thomson Forbes, David T. Davies, Frank E. Blaney, Wyman Paul Adrian, and Graham J. Riley, Guy A. Kennett, Fiona Bailey
Publikováno v:
Journal of Medicinal Chemistry. 41:1598-1612
The synthesis, biological activity, and molecular modeling of a novel series of substituted 1-(3-pyridylcarbamoyl)indolines are reported. These compounds are isosteres of the previously published indole urea 1 (SB-206553) and illustrate the use of ar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a2bc69439419d750f0f653013b882dd
https://doi.org/10.1021/jm970741j
https://doi.org/10.1021/jm970741j
Autor:
Mark James Bamford, Andrew R. Calver, David Matthew Wilson, Rebecca K. Davis, Nicholas Bailey, Isabel Jm Beresford, Jason Witherington, Susannah Davis, Jon Graham Anthony Steadman, Phillip Jeffrey, Vicky Holland, Joanne Schogger, Christopher A. Parr, Jeffrey Wald, Teresa Heslop, Michael A. Briggs, Terrance A. Panchal, Leanne Harris, Andrew D. Medhurst, Kim Brackenborough, David Kenneth Dean, Tania O. Stean, Brenda K. Trail, Nigel Quashie, Angela Worby, Stephen J. Brough, Barry Crook, James Apps, Andrew K. Takle, Robert P. Davis, Sanjeet Singh Sehmi
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(24)
This Letter describes the discovery of GSK189254 and GSK239512 that were progressed as clinical candidates to explore the potential of H3 receptor antagonists as novel therapies for the treatment of Alzheimer's disease and other dementias. By careful
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e541fa0f8606fd8aa20c773c236c2d64
https://pubmed.ncbi.nlm.nih.gov/24269482
https://pubmed.ncbi.nlm.nih.gov/24269482
Autor:
Stephen J. Medhurst, Sandra Arpino, James Wright, Darren Jason Mitchell, Alexander J. Stevens, James Biggs, Kim Winborn, Susan Marie Westaway, John B. Davis, Jeffrey C. Jerman, Vicky Holland, Tanya Coleman, Jennifer E. Cryan, Geoffrey Stemp, Sarah C. Lappin, Jon T. Seal, Harshad Kantilal Rami, Leontine Saskia Trouw, Mervyn Thompson, Martin J. Gunthorpe
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(20)
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87b365ea545812a5b73fbe175229b22f
https://pubmed.ncbi.nlm.nih.gov/18809327
https://pubmed.ncbi.nlm.nih.gov/18809327
N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1
Autor:
Harshad Kantilal Rami, Mervyn Thompson, John B. Davis, Geoffrey Stemp, Jeffrey C. Jerman, Kim Winborn, Ying-Kit Chung, Alexander J. Stevens, Susan Marie Westaway, Stephen J. Medhurst, James Wright, Vicky Holland
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(17)
Starting from the high throughput screening hit (3), novel N-tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl carboxamides have been identified as potent antagonists of the ion channel TRPV1. The N-quinolinylnicotinamide (46) showed excellent p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::141036e0f6f1177a85d4e09fef34cda7
https://pubmed.ncbi.nlm.nih.gov/16806913
https://pubmed.ncbi.nlm.nih.gov/16806913