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Angus Murray Macleod
Researcher at Merck & Co.
Publications - 145
Citations - 4487
Angus Murray Macleod is an academic researcher from Merck & Co.. The author has contributed to research in topics: Receptor & Agonist. The author has an hindex of 39, co-authored 145 publications receiving 4369 citations. Previous affiliations of Angus Murray Macleod include Merck Sharp & Dohme Federal Credit Union & University of Hertfordshire.
Papers
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Journal ArticleDOI
An Inverse Agonist Selective for α5 Subunit-Containing GABAA Receptors Enhances Cognition
Gerard R. Dawson,Karen A. Maubach,Neil Collinson,M. Cobain,B. J. Everitt,Angus Murray Macleod,Hedaythul Choudhury,L. M. McDonald,Goplan V. Pillai,W. Rycroft,Alison J. Smith,F. Sternfeld,F. D. Tattersall,Keith A. Wafford,David S. Reynolds,Guy R. Seabrook,John R. Atack +16 more
TL;DR: The 5-subunit GABAA receptor was found to be a novel target for the development of selective inverse agonists with utility in the treatment of disorders associated with a cognitive deficit as mentioned in this paper.
Journal ArticleDOI
Tachykinin NK1 receptor antagonists act centrally to inhibit emesis induced by the chemotherapeutic agent cisplatin in ferrets.
F.D. Tattersall,W. Rycroft,Barbara Francis,David Pearce,Kevin John Merchant,Angus Murray Macleod,T. Ladduwahetty,Linda Elizabeth Keown,Christopher John Swain,R. Baker,Margaret A. Cascieri,E. Ber,Joseph M. Metzger,D. E. Macintyre,Raymond G. Hill,Richard Hargreaves +15 more
TL;DR: It is shown that brain penetration is essential for the anti-emetic action of systemically administered NK1 receptor antagonists with and without brain penetration to central NK1 receptors sites.
Patent
Heterocyclic compounds, processes for their preparation and pharmaceutical compositions containing them
TL;DR: In this paper, an optional covalent bond is defined, where one of X and Y is H and the other is hydroxy or C?1-6?alkoxy, or X and y are together = 0 or =NOR?5; R1 and R2? are H; R3 is H, C? 1-6-alkyl or C2-6alkenyl; and R?4? is phenyl.
Journal ArticleDOI
Identification of a Novel, Selective GABAA α5 Receptor Inverse Agonist Which Enhances Cognition
Mark Stuart Chambers,John R. Atack,Howard B. Broughton,Neil Collinson,Susan M. Cook,Gerard R. Dawson,Sarah Christine Hobbs,George R. Marshall,Karen A. Maubach,Goplan V. Pillai,and Austin J. Reeve,Angus Murray Macleod +11 more
TL;DR: 6,6-Dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro- 2-benzothiophen-4(5H)-one (43) has been identified as a full inverse agonist at the GABAA α5 receptor and is functionally selective over the other major GAB AA receptor subtypes.
Journal ArticleDOI
Novel quinuclidine-based ligands for the muscarinic cholinergic receptor
John Saunders,Mark Cassidy,Stephen B. Freedman,E. A. Harley,Leslie L. Iversen,C. Kneen,Angus Murray Macleod,Kevin John Merchant,Roger J. Snow,Raymond Baker +9 more
TL;DR: The design, synthesis, and biochemical characterization of novel quinuclidine-based muscarinic agonists which can readily penetrate into the central nervous system and which are capable of displaying high efficacy at cortical sites are described.