Search Results - "Carling, Robert W"

A Second Generation Prostanoid Receptor Antagonist Acting at Multiple Receptor Subtypes by Woodward, David F, Wang, Jenny W, Spada, Clayton S, Carling, Robert W, Martos, Jose L, Pettit, Simon, Kangasmetsa, Jussi, Waterbury, L. David, Lawrence, Matthew, Hu, Wenzheng, Poloso, Neil J

“…It has previously been reported that a prototypical compound (AGN 211377), which blocks pro-inflammatory prostanoid receptors (DP1, DP2, EP1, EP4, FP, TP) and…”
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In vivo studies validating multitargeting of prostanoid receptors for achieving superior anti‐inflammatory effects by Woodward, David F., Wang, Jenny W., Ni, Ming, Bauer, Alex, Martos, Jose L., Carling, Robert W., Poloso, Neil J.

“…The purpose of these studies was to test the hypothesis that a selected polypharmacological approach for treating the prostanoid‐mediated component of…”
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Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists by Rowley, Michael, Kulagowski, Janusz J, Watt, Alan P, Rathbone, Denise, Stevenson, Graeme I, Carling, Robert W, Baker, Raymond, Marshall, George R, Kemp, John A, Foster, Alan C, Grimwood, Sarah, Hargreaves, Richard, Hurley, Catherine, Saywell, Kay L, Tricklebank, Mark D, Leeson, Paul D

“…A major issue in designing drugs as antagonists at the glycine site of the NMDA receptor has been to achieve good in vivo activity. A series of…”
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Multitargeting of selected prostanoid receptors provides agents with enhanced anti‐inflammatory activity in macrophages by Wang, Jenny W., Woodward, David F., Martos, Jose L., Cornell, Clive L., Carling, Robert W., Kingsley, Philip J., Marnett, Lawrence J.

“…ABSTRACT A polypharmacologic approach to prostanoid based anti‐inflammatory therapeutics was undertaken in order to exploit both the anti‐ and proinflammatory…”
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FAAH-Catalyzed C–C Bond Cleavage of a New Multitarget Analgesic Drug by Ligresti, Alessia, Silvestri, Cristoforo, Vitale, Rosa Maria, Martos, Jose L, Piscitelli, Fabiana, Wang, Jenny W, Allarà, Marco, Carling, Robert W, Luongo, Livio, Guida, Francesca, Illiano, Anna, Amoresano, Angela, Maione, Sabatino, Amodeo, Pietro, Woodward, David F, Di Marzo, Vincenzo, Marino, Gennaro

“…The discovery of extended catalytic versatilities is of great importance in both the chemistry and biotechnology fields. Fatty acid amide hydrolase (FAAH)…”
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Cellular basis for bimatoprost effects on human conventional outflow by Stamer, W Daniel, Piwnica, David, Jolas, Thierry, Carling, Robert W, Cornell, Clive L, Fliri, Hans, Martos, Jose, Pettit, Simon N, Wang, Jenny W, Woodward, David F

“…Bimatoprost is a widely used ocular hypotensive agent to treat glaucoma. It lowers intraocular pressure in humans by increasing both pressure-independent…”
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4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor by Leeson, Paul D, Carling, Robert W, Moore, Kevin W, Moseley, Angela M, Smith, Julian D, Stevenson, Graeme, Chan, Tony, Baker, Raymond, Foster, Alan C

“…trans-2-Carboxy-5,7-dichloro-4-amidotetrahydroquinolines, evolved from the lead 5,7-dichlorokynurenic acid, have been synthesized and tested for in vitro…”
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3-Phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and Analogues:  High-Affinity γ-Aminobutyric Acid-A Benzodiazepine Receptor Ligands with α2, α3, and α5-Subtype Binding Selectivity over α1 by Carling, Robert W, Moore, Kevin W, Street, Leslie J, Wild, Deborah, Isted, Catherine, Leeson, Paul D, Thomas, Steven, O'Connor, Desmond, McKernan, Ruth M, Quirk, Katherine, Cook, Susan M, Atack, John R, Wafford, Keith A, Thompson, Sally A, Dawson, Gerard R, Ferris, Pushpinder, Castro, José L

“…Studies with our screening lead 5 and the literature compound 6 led to the identification of 6-benzyloxy-3-(4-methoxy)phenyl-1,2,4-triazolo[3,4-a]phthalazine 8…”
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An Orally Bioavailable, Functionally Selective Inverse Agonist at the Benzodiazepine Site of GABAA α5 Receptors with Cognition Enhancing Properties by Chambers, Mark S, Atack, John R, Carling, Robert W, Collinson, Neil, Cook, Susan M, Dawson, Gerard R, Ferris, Pushpindar, Hobbs, Sarah C, O'Connor, Desmond, Marshall, George, Rycroft, W, MacLeod, Angus M

“…(3-tert-Butyl-7-(5-methylisoxazol-3-yl)-2-(1-methyl-1H-1,2,4-triazol-5-ylmethoxy)pyrazolo[1,5-d][1,2,4]triazine (13) has been identified as a functionally…”
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Selective, Orally Active γ-Aminobutyric AcidA α5 Receptor Inverse Agonists as Cognition Enhancers by Sternfeld, Francine, Carling, Robert W, Jelley, Richard A, Ladduwahetty, Tamara, Merchant, Kevin J, Moore, Kevin W, Reeve, Austin J, Street, Leslie J, O'Connor, Desmond, Sohal, Bindi, Atack, John R, Cook, Susan, Seabrook, Guy, Wafford, Keith, Tattersall, F. David, Collinson, Neil, Dawson, Gerard R, Castro, José L, MacLeod, Angus M

“…Nonselective inverse agonists at the γ-aminobutyric acidA (GABA-A) benzodiazepine binding site have cognition-enhancing effects in animals but are anxiogenic…”
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Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor by Leeson, Paul D, Baker, Raymond, Carling, Robert W, Curtis, Neil R, Moore, Kevin W, Williams, Brian J, Foster, Alan C, Donald, Angus E, Kemp, John A, Marshall, George R

“…Derivatives of the nonselective excitatory amino acid antagonist kynurenic acid (4-oxo-1,4-dihydroquinoline-2-carboxylic acid, 1) have been synthesized and…”
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Discovery of Functionally Selective 7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABAA Receptor Agonists at the α3 Subunit by Russell, Michael G. N, Carling, Robert W, Atack, John R, Bromidge, Frances A, Cook, Susan M, Hunt, Peter, Isted, Catherine, Lucas, Matt, McKernan, Ruth M, Mitchinson, Andrew, Moore, Kevin W, Narquizian, Robert, Macaulay, Alison J, Thomas, David, Thompson, Sally-Anne, Wafford, Keith A, Castro, José L

“…We have previously identified the 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazine (1) as a potent partial agonist for the α3 receptor subtype…”
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Synthesis and Biological Evaluation of 3-Heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and Analogues as Subtype-Selective Inverse Agonists for the GABAAα5 Benzodiazepine Binding Site by Street, Leslie J, Sternfeld, Francine, Jelley, Richard A, Reeve, Austin J, Carling, Robert W, Moore, Kevin W, McKernan, Ruth M, Sohal, Bindi, Cook, Susan, Pike, Andrew, Dawson, Gerard R, Bromidge, Frances A, Wafford, Keith A, Seabrook, Guy R, Thompson, Sally A, Marshall, George, Pillai, Goplan V, Castro, José L, Atack, John R, MacLeod, Angus M

“…The identification of a novel series of 7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines as GABAAα5 inverse agonists, which have both…”
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Discovery of Imidazo[1,2-b][1,2,4]triazines as GABAA α2/3 Subtype Selective Agonists for the Treatment of Anxiety by Russell, Michael G. N, Carling, Robert W, Street, Leslie J, Hallett, David J, Goodacre, Simon, Mezzogori, Elena, Reader, Michael, Cook, Susan M, Bromidge, Frances A, Newman, Robert, Smith, Alison J, Wafford, Keith A, Marshall, George R, Reynolds, David S, Dias, Rebecca, Ferris, Pushpindar, Stanley, Jo, Lincoln, Rachael, Tye, Spencer J, Sheppard, Wayne F. A, Sohal, Bindi, Pike, Andrew, Dominguez, Maria, Atack, John R, Castro, José L

“…The identification of a series of imidazo[1,2-b][1,2,4]triazines with high affinity and functional selectivity for the GABAA α3-containing receptor subtype is…”
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7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4- triazol-3-ylmethoxy)-3-(2-fluorophenyl)- 1,2,4-triazolo[4,3-b]pyridazine:  A Functionally Selective γ-Aminobutyric AcidA (GABAA) α2/α3-Subtype Selective Agonist That Exhibits Potent Anxiolytic Activity but Is Not Sedating in Animal Models by Carling, Robert W, Madin, Andrew, Guiblin, Alec, Russell, Michael G. N, Moore, Kevin W, Mitchinson, Andrew, Sohal, Bindi, Pike, Andrew, Cook, Susan M, Ragan, Ian C, McKernan, Ruth M, Quirk, Kathleen, Ferris, Pushpinder, Marshall, George, Thompson, Sally Ann, Wafford, Keith A, Dawson, Gerard R, Atack, John R, Harrison, Timothy, Castro, José L, Street, Leslie J

“…There is increasing evidence that compounds with selectivity for γ-aminobutyric acidA (GABAA) α2- and/or α3-subtypes may retain the desirable anxiolytic…”
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N',2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists by ELLIOTT, Jason M, CARTING, Robert W, MURRAY, Fraser, RIGBY, Michael, ROYO, Inmaculada, RUSSELL, Michael G. N, SOHAL, Bindi, KWEI LAN TSAO, WILLIAMS, Brian, CHAMBERS, Mark, CHICCHI, Gary G, HUTSON, Peter H, JONES, A. Brian, MACLEOD, Angus, MARWOOD, Rose, MENESES-LORENTE, Georgina, MEZZOGORI, Elena

“…A new class of potent NK3R antagonists based on the N',2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound…”
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Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as α2/α3 subtype selective GABAA agonists for the treatment of anxiety by Goodacre, Simon C., Hallett, David J., Carling, Robert W., Castro, José L., Reynolds, David S., Pike, Andrew, Wafford, Keith A., Newman, Robert, Atack, John R., Street, Leslie J.

“…Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABAA agonists. Compound 16d has…”
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N',2-Diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II by ELLIOTT, Jason M, CARTING, Robert W, MURRAY, Fraser, RIGBY, Michael, ROYO, Inmaculada, RUSSELL, Michael G. N, SHAW, Duncan, SOHAL, Bindi, KWEI LAN TSAO, WILLIAMS, Brian, CHICCHI, Gary G, CRAWFORTH, James, HUTSON, Peter H, JONES, A. Brian, KELLY, Sarah, MARWOOD, Rose, MENESES-LORENTE, Georgina, MEZZOGORI, Elena

“…Introduction of selected amine containing side chains into the 3-position of N',2-diphenylquinoline-4-carbohydrazide based NK3 antagonists abolishes unwanted…”
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2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: Functionally selective GABAA α3-subtype agonists by Carling, Robert W., Russell, Michael G.N., Moore, Kevin W., Mitchinson, Andrew, Guiblin, Alexander, Smith, Alison, Wafford, Keith A., Marshall, George, Atack, John R., Street, Leslie J.

“…Novel synthetic routes have been devised for the preparation of previously inaccessible 2,3,7-trisubstituted pyrazolo[1,5-d][1,2,4]triazines 2. These compounds…”
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2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor by MITCHINSON, Andrew, ATACK, John R, NARQUIZIAN, Robert, SMITH, Alison, STREET, Leslie J, THOMPSON, Sally-Anne, WAFFORD, Keith, BLURTON, Peter, CARLING, Robert W, CASTRO, José L, CURLEY, Karen S, RUSSELL, Michael G. N, MARSHALL, George, MCKERNAN, Ruth M, MOORE, Kevin W

“…2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones are GABAA receptor benzodiazepine binding site ligands with functional selectivity for the alpha3 subtype over the…”
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