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15 results on '"Crook, Barry"'

1. Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats

Author

Medhurst, Andrew D., Briggs, Michael A., Bruton, Gordon, Calver, Andrew R., Chessell, Iain, Crook, Barry, Davis, John B., Davis, Robert P., Foley, Andrew G., Heslop, Teresa, Hirst, Warren D., Medhurst, Stephen J., Ociepka, Sandrine, Ray, Alison, Regan, Ciaran M., Sargent, Becky, Schogger, Joanne, Stean, Tania O., Trail, Brenda K., Upton, Neil, White, Trevor, Orlek, Barry, and Wilson, David M.

Published
2007
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2. Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists

Author

Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Brackenborough, Kim, Briggs, Michael A., Brough, Stephen, Calver, Andrew R., Crook, Barry, Davis, Rebecca K., Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heslop, Teresa, Holland, Vicky, Jeffrey, Phillip, Panchal, Terrance A., Parr, Christopher A., Quashie, Nigel, Schogger, Joanne, Sehmi, Sanjeet S., Stean, Tania O., Steadman, Jon G.A., Trail, Brenda, Wald, Jeffrey, Worby, Angela, Takle, Andrew K., Witherington, Jason, and Medhurst, Andrew D.

Published
2013
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3. The discovery of the benzazepine class of histamine H3 receptor antagonists

Author

Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Briggs, Michael A., Calver, Andrew R., Crook, Barry, Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heightman, Tom D., Panchal, Terry, Parr, Christopher A., Quashie, Nigel, Steadman, Jon G.A., Schogger, Joanne, Sehmi, Sanjeet S., Stean, Tania O., Takle, Andrew K., Trail, Brenda K., White, Trevor, Witherington, Jason, Worby, Angela, and Medhurst, Andrew D.

Published
2013
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4. GSK189254, a Novel H3 Receptor Antagonist That Binds to Histamine H3 Receptors in Alzheimer's Disease Brain and Improves Cognitive Performance in Preclinical Models

Author

Medhurst, Andrew D., primary, Atkins, Alan R., additional, Beresford, Isabel J., additional, Brackenborough, Kim, additional, Briggs, Michael A., additional, Calver, Andrew R., additional, Cilia, Jackie, additional, Cluderay, Jane E., additional, Crook, Barry, additional, Davis, John B., additional, Davis, Rebecca K., additional, Davis, Robert P., additional, Dawson, Lee A., additional, Foley, Andrew G., additional, Gartlon, Jane, additional, Gonzalez, M. Isabel, additional, Heslop, Teresa, additional, Hirst, Warren D., additional, Jennings, Carol, additional, Jones, Declan N. C., additional, Lacroix, Laurent P., additional, Martyn, Abbe, additional, Ociepka, Sandrine, additional, Ray, Alison, additional, Regan, Ciaran M., additional, Roberts, Jennifer C., additional, Schogger, Joanne, additional, Southam, Eric, additional, Stean, Tania O., additional, Trail, Brenda K., additional, Upton, Neil, additional, Wadsworth, Graham, additional, Wald, Jeffrey A., additional, White, Trevor, additional, Witherington, Jason, additional, Woolley, Marie L., additional, Worby, Angela, additional, and Wilson, David M., additional

Published
2007
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5. O3-05-01

Author

Medhurst, Andrew D., primary, Crook, Barry, additional, Ociepka, Sandrine, additional, Davies, Robert P., additional, Calver, Andrew, additional, Ray, Alison, additional, Stean, Tania, additional, Trail, Brenda, additional, Wadsworth, Graham, additional, Brackenborough, Kim, additional, Davis, Rebecca K., additional, Gonzalez, M. Isabel, additional, Virley, David, additional, Smith, Martin, additional, Roberts, Jennifer, additional, Ahmed, Sharlin, additional, Heslop, Teresa, additional, Schogger, Joanne, additional, White, Trevor, additional, Briggs, Michael, additional, Wald, Jeffrey, additional, Foley, Andrew, additional, Regan, Ciaran, additional, Witherington, Jason, additional, and Wilson, David M., additional

Published
2006
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6. TRPM2 Is Elevated in the tMCAO Stroke Model, Transcriptionally Regulated, and Functionally Expressed in C13 Microglia

Author

FONFRIA, ELENA, primary, MATTEI, CESAR, additional, HILL, KERSTIN, additional, BROWN, JON T., additional, RANDALL, ANDREW, additional, BENHAM, CHRISTOPHER D., additional, SKAPER, STEPHEN D., additional, CAMPBELL, COLIN A., additional, CROOK, BARRY, additional, MURDOCK, PAUL R., additional, WILSON, JENNIFER M., additional, MAURIO, FRANK P., additional, OWEN, DAVINA E., additional, TILLING, PAULA L., additional, and MCNULTY, SHAUN, additional

Published
2006
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8. Alteration in Brain Presenilin 1 mRNA Expression in Early Onset Familial Alzheimer's Disease

Author

Barton, Amanda J.L., primary, Crook, Barry W., additional, Karran, Eric H., additional, Brown, Frank, additional, Dewar, Deborah, additional, Mann, David M.A., additional, Pearson, R.Carl A., additional, Graham, David I., additional, Hardy, John, additional, Hutton, Mike, additional, Duff, Karen, additional, Goate, Alison M., additional, Clark, Robert F., additional, and Roberts, Gareth W., additional

Published
1996
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10. O3-05-01: GSK189254 - a novel H3 receptor antagonist that binds to H3 receptors in the human brain and improves cognitive performance in preclinical models

Author

Medhurst, Andrew D., Crook, Barry, Ociepka, Sandrine, Davies, Robert P., Calver, Andrew, Ray, Alison, Stean, Tania, Trail, Brenda, Wadsworth, Graham, Brackenborough, Kim, Davis, Rebecca K., Gonzalez, M. Isabel, Virley, David, Smith, Martin, Roberts, Jennifer, Ahmed, Sharlin, Heslop, Teresa, Schogger, Joanne, White, Trevor, Briggs, Michael, Wald, Jeffrey, Foley, Andrew, Regan, Ciaran, Witherington, Jason, and Wilson, David M.

Published
2006
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11. letters.

Author

Dorn, Jonathan, Neilson, Sean, Kimball, Don, Budlong, Tom, and Crook, Barry R.

Subjects
LETTERS to the editor, BACKPACKING, PACK transportation
Abstract

Presents letters to the editor referencing articles and topics discussed in previous issues. "Writers on the Range," column by Sean Neilson, which deals with the Yellowstone National Park; Essence of backpacking; Budget shortfall in the U.S. National Park Service.

Published
2004

12. letters.

Author

Tillotson, David, Essen, Deb, Crook, Barry, Christmas, Carrie, and Kaliche, Kali

Subjects
LETTERS to the editor, CONSERVATIONISTS, LEGISLATIVE power, JUDGES, LAND use
Abstract

Presents letters to the editor referencing to articles and topics discussed in previous issues of the periodical "High Country News." Reason behind the failure of the conservation movement to gain support from Republicans; Usurpation of legislative power by federal judges; "Arizona Land Swap Dogged by Questions," which discussed the Yavapai Ranch land exchange.

Published
2004

13. The discovery of the benzazepine class of histamine H3 receptor antagonists.

Author

Wilson, David M., Apps, James, Bailey, Nicholas, Bamford, Mark J., Beresford, Isabel J., Briggs, Michael A., Calver, Andrew R., Crook, Barry, Davis, Robert P., Davis, Susannah, Dean, David K., Harris, Leanne, Heightman, Tom D., Panchal, Terry, Parr, Christopher A., Quashie, Nigel, Steadman, Jon G.A., Schogger, Joanne, Sehmi, Sanjeet S., and Stean, Tania O.

Subjects
*BENZAZEPINES, *HISTAMINE, *ANTIHISTAMINES, *PHARMACODYNAMICS, *DRUG development, *PHARMACEUTICAL chemistry
Abstract

Abstract: This Letter describes the discovery of a novel series of H3 receptor antagonists. The initial medicinal chemistry strategy focused on deconstructing and simplifying an early screening hit which rapidly led to the discovery of a novel series of H3 receptor antagonists based on the benzazepine core. Employing an H3 driven pharmacodynamic model, the series was then further optimised through to a lead compound that showed robust in vivo functional activity and possessed overall excellent developability properties. [Copyright &y& Elsevier]

Published
2013
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14. Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats

Author

Medhurst, Andrew D., Briggs, Michael A., Bruton, Gordon, Calver, Andrew R., Chessell, Iain, Crook, Barry, Davis, John B., Davis, Robert P., Foley, Andrew G., Heslop, Teresa, Hirst, Warren D., Medhurst, Stephen J., Ociepka, Sandrine, Ray, Alison, Regan, Ciaran M., Sargent, Becky, Schogger, Joanne, Stean, Tania O., Trail, Brenda K., and Upton, Neil

Subjects
*MEMORY disorders, *DRUG receptors, *DRUG development, *CLINICAL medicine
Abstract

Abstract: GSK207040 (5-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-2-pyrazinecarboxamide) and GSK334429 (1-(1-methylethyl)-4-({1-[6-(trifluoromethyl)-3-pyridinyl]-4-piperidinyl}carbonyl)hexahydro-1H-1,4-diazepine) are novel and selective non-imidazole histamine H3 receptor antagonists from distinct chemical series with high affinity for human (pK i =9.67±0.06 and 9.49±0.09, respectively) and rat (pK i =9.08±0.16 and 9.12±0.14, respectively) H3 receptors expressed in cerebral cortex. At the human recombinant H3 receptor, GSK207040 and GSK334429 were potent functional antagonists (pA2 =9.26±0.04 and 8.84±0.04, respectively versus H3 agonist-induced changes in cAMP) and exhibited inverse agonist properties (pIC50 =9.20±0.36 and 8.59±0.04 versus basal GTPγS binding). Following oral administration, GSK207040 and GSK334429 potently inhibited cortical ex vivo [3H]-R-α-methylhistamine binding (ED50 =0.03 and 0.35mg/kg, respectively). Functional antagonism of central H3 receptors was demonstrated by blockade of R-α-methylhistamine-induced dipsogenia in rats (ID50 =0.02 and 0.11mg/kg p.o. for GSK207040 and GSK334429, respectively). In more pathophysiologically relevant pharmacodynamic models, GSK207040 (0.1, 0.3, 1 and 3mg/kg p.o.) and GSK334429 (0.3, 1 and 3mg/kg p.o.) significantly reversed amnesia induced by the cholinergic antagonist scopolamine in a passive avoidance paradigm. In addition, GSK207040 (0.1, 0.3 and 1mg/kg p.o.) and GSK334429 (3 and 10mg/kg p.o.) significantly reversed capsaicin-induced reductions in paw withdrawal threshold, suggesting for the first time that blockade of H3 receptors may be able to reduce tactile allodynia. Novel H3 receptor antagonists such as GSK207040 and GSK334429 may therefore have therapeutic potential not only in dementia but also in neuropathic pain. [Copyright &y& Elsevier]

Published
2007
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