G
Graeme Irvine Stevenson
Researcher at Merck & Co.
Publications - 34
Citations - 1925
Graeme Irvine Stevenson is an academic researcher from Merck & Co.. The author has contributed to research in topics: Indole test & Glycine. The author has an hindex of 24, co-authored 34 publications receiving 1887 citations. Previous affiliations of Graeme Irvine Stevenson include Merck Sharp & Dohme Federal Credit Union.
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Journal ArticleDOI
L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity.
Mark S. Shearman,Dirk Beher,Earl E. Clarke,Huw D. Lewis,Timothy Harrison,Peter W. Hunt,Alan Nadin,Adrian L. Smith,Graeme Irvine Stevenson,José L. Castro +9 more
TL;DR: The identification of L-685,458 is reported as a structurally novel inhibitor of AβPP γ-secretase activity, with a similar potency for Alzheimer's disease targeting the N- and C-termini of the Aβ peptide.
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4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor.
Paul D. Leeson,Robert W. Carling,K W Moore,A M Moseley,Julian D. Smith,Graeme Irvine Stevenson,T Chan,R. Baker,Alan C. Foster,Sarah Grimwood +9 more
TL;DR: Molecular modeling studies show that the 4-carbonyl groups of the kynurenic acids, the tetrahydroquinolines, and related antagonists based on N-(chlorophenyl)glycine, can interact with a single putative H-bond donor on the receptor.
Journal ArticleDOI
Novel 5-HT3 antagonists. Indole oxadiazoles.
Christopher John Swain,Raymond Baker,C. Kneen,J. D. Moseley,John Saunders,Eileen Mary Seward,Graeme Irvine Stevenson,Margaret S. Beer,Josephine A. Stanton,K. Watling +9 more
TL;DR: Results have been incorporated into a proposed binding model for the 5-HT3 antagonist binding site, in which the optimum distance between the aromatic binding site and the basic amine is 8.4-8.9 A and the steric limitations are defined by van der Waals difference mapping.
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Effect of plasma protein binding on in vivo activity and brain penetration of glycine/NMDA receptor antagonists.
Michael Rowley,Janusz Jozef Kulagowski,Alan P. Watt,Denise Rathbone,Graeme Irvine Stevenson,Robert W. Carling,Raymond Baker,George R. Marshall,John A. Kemp,Alan C. Foster,Sarah Grimwood,Richard Hargreaves,Catherine Hurley,K. L. Saywell,Mark D. Tricklebank,Paul D. Leeson +15 more
TL;DR: It is shown that binding of the compounds to plasma protein limits their brain penetration, and it is suggested that it is necessary to either keep log P low or pKa high to obtain good central nervous system activity.
Journal ArticleDOI
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.
Michael Rowley,Paul D. Leeson,Graeme Irvine Stevenson,A M Moseley,Ian Stansfield,I. Sanderson,L. Robinson,R. Baker,John A. Kemp,George R. Marshall +9 more
TL;DR: Novel antagonists at the glycine site of the NMDA receptor have been designed in which the anionic functionality is a vinylogous acid, in the form of a 4-hydroxyquinolin-2(1H)-one, which was tested for their ability to prevent audiogenic seizure in DBA/2 mice.