Search Results - "Stevenson, G I"

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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Serine derived NK1 antagonists 2 : A pharmacophore model for arylsulfonamide binding by ELLIOTT, J. M, BROUGHTON, H, CASCIERI, M. A, CHICCHI, G, HUSCROFT, I. T, KURTZ, M, MACLEOD, A. M, SADOWSKI, S, STEVENSON, G. I

“…Modifications to the spirocyclic aryl sulfonamide portion of serine derived NK1 antagonists allow a partial pharmacophore model to be developed…”
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3-Acyl-4-hydroxyquinolin-2(1H)-ones. Systemically active anticonvulsants acting by antagonism at the glycine site of the N-methyl-D-aspartate receptor complex by Rowley, Michael, Leeson, Paul D, Stevenson, Graeme I, Moseley, Angela M, Stansfield, Ian, Sanderson, Ian, Robinson, Lesley, Baker, Raymond, Kemp, John A

“…Most full antagonists at the glycine site of the NMDA receptor contain a carboxylic acid, which we believe to be detrimental to penetration of the blood-brain…”
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Novel 5-HT3 antagonists: indol-3-ylspiro(azabicycloalkane-3,5'(4'H)oxazoles) by Swain, C. J, Baker, R, Kneen, C, Herbert, R, Moseley, J, Saunders, J, Seward, E. M, Stevenson, G. I, Beer, M

“…The synthesis and biochemical evaluation of a series of spirofused indole oxazoline 5-HT3 antagonists is described in which the oxazoline ring acts as a…”
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Serine derived NK1 antagonists 1 : The effect of modifications to the serine substituents by ELLIOTT, J. M, CASCIERI, M. A, SADOWSKI, S, STEVENSON, G. I, CHICCHI, G, DAVIES, S, KELLEHER, F. J, KURTZ, M, LADDUWAHETTY, T, LEWIS, R. T, MACLEOD, A. M, MERCHANT, K. J

“…A series of novel serine derived NK1 antagonists is described. The effect of variations in the N-benzyl, O-benzyl and serine groups are used to define the…”
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4,4-Disubstituted Piperidine High-Affinity NK1 Antagonists:  Structure−Activity Relationships and in Vivo Activity by Stevenson, Graeme I, Huscroft, Ian, MacLeod, Angus M, Swain, Christopher J, Cascieri, Margaret A, Chicchi, Gary G, Graham, Michael I, Harrison, Timothy, Kelleher, Fintan J, Kurtz, Marc, Ladduwahetty, Tamara, Merchant, Kevin J, Metzger, Joseph M, MacIntyre, D. E, Sadowski, Sharon, Sohal, Balbinder, Owens, Andrew P

“…Previously reported studies from these laboratories described the design of a novel series of high-affinity NK1 antagonists based on the 4,4-disubstituted…”
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4,4-Disubstituted piperidines : a new class of NK1 antagonist by STEVENSON, G. I, MACLEOD, A. M, HUSCROFT, I, CASCIERI, M. A, SADOWSKI, S, BAKER, R

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2-Aryl tryptamines : Selective high-affinity antagonists for the h5-HT2A receptor by STEVENSON, Graeme I, SMITH, Adrian L, LEWIS, Stephen, MICHIE, Stephen G, NEDUVELIL, Joseph G, PATEL, Smita, MARWOOD, Rosemarie, PATEL, Shil, CASTRO, José L

“…A series of 2-aryl tryptamines have been identified as high-affinity h5-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A…”
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Solid-phase synthesis of 2,3-disubstituted indoles : Discovery of a novel, high-affinity, selective h5-HT2A antagonist by SMITH, Adrian L, STEVENSON, Graeme I, LEWIS, Stephen, PATEL, Smita, CASTRO, José L

“…The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification…”
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Purification of the 5-hydroxytryptamine 5-HT3 receptor from NCB20 cells by McKernan, R M, Gillard, N P, Quirk, K, Kneen, C O, Stevenson, G I, Swain, C J, Ragan, C I

“…A 5-hydroxytryptamine 5-HT3 receptor binding site has been purified from deoxycholate-solubilized NCB20 cell membranes. Purification (1,700-fold) was achieved…”
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An Efficient Protocol for the Preparation of Primary Alcohols Bearing a β-Chiral Center via an Oxazolidinone Auxiliary Mediated Resolution, and Application to the Synthesis of 4,4-Disubstituted Piperidine Substance P Antagonists by Lewis, Richard T, Ladduwahetty, Tamara, Merchant, Kevin J, Keown, Linda E, Hitzel, Laure, Verrier, Hugh, Stevenson, Graeme I, MacLeod, Angus M

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Traceless solid phase synthesis of 2,3-disubstituted indoles by Smith, Adrian L., Stevenson, Graeme I., Swain, Christopher J., Castro, JoséL.

“…An efficient method for the traceless solid phase synthesis of 2,3-disubstituted indoles using a THP linker and a Pd(0)-mediated annulation of 2-iodoaniline…”
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A novel series of potent γ-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core by Lewis, Stephen J., Smith, Adrian L., Neduvelil, Joseph G., Stevenson, Graeme I., Lindon, Matthew J., Jones, A. Brian, Shearman, Mark S., Beher, Dirk, Clarke, Earl, Best, Jonathan D., Peachey, James E., Harrison, Timothy, Castro, J. Luis

“…[Display omitted] A new series of γ-secretase inhibitors was developed from an in-house screening hit based on a benzobicyclo[4.2.1]nonane core. Lead…”
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Purification of the 5-hydorxytryptamine 5-HT3 receptor from NCB20 cells by MCKERNAN, R. M, GILLARD, N. P, QUIRK, K, KNEEN, C. O, STEVENSON, G. I, SWAIN, C. J, RAGAN, C. I

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Purification of the 5-hydroxytryptamine 5-HT sub(3) receptor from NCB20 cells by McKernan, R M, Gillard, N P, Quirk, K, Kneen, C O, Stevenson, GI, Swain, C J, Ragan, C I

“…A 5-hydroxytryptamine 5-HT sub(3) receptor binding site has been purified from deoxycholate-solubilized NCB20 cell membranes. Purification (1,700-fold) was…”
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