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Alan P. Watt
Researcher at Merck & Co.
Publications - 54
Citations - 2464
Alan P. Watt is an academic researcher from Merck & Co.. The author has contributed to research in topics: Enantiomer & Receptor. The author has an hindex of 25, co-authored 53 publications receiving 2393 citations. Previous affiliations of Alan P. Watt include Rockefeller University.
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Journal ArticleDOI
Drug-protein adducts: an industry perspective on minimizing the potential for drug bioactivation in drug discovery and development.
TL;DR: This paper serves to provide one pragmatic approach to addressing the issue of bioactivation from an industry viewpoint based on protocols adopted by Merck Research Laboratories.
Journal Article
Biological Profile of L-745,870, a Selective Antagonist with High Affinity for the Dopamine D4 Receptor
Shil Patel,Stephen B. Freedman,K. L. Chapman,F. Emms,A. E. Fletcher,M.R. Knowles,R. Marwood,G. Mcallister,J Myers,N. Curtis,Janusz Jozef Kulagowski,Paul D. Leeson,M. Ridgill,Michael I. Graham,S. Matheson,Denise Rathbone,Alan P. Watt,Linda J. Bristow,N. M. J. Rupniak,E. Baskin,Joseph J. Lynch,C I Ragan +21 more
TL;DR: Results show that dopamine D4 receptor antagonism in the brain does not result in the same neurochemical consequences (increased dopamine metabolism or hyperprolactinemia) observed with typical neuroleptics.
Journal ArticleDOI
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
Total Synthesis and Determination of the Absolute Configuration of Epibatidine
Stephen Robert Fletcher,Raymond Baker,Mark Stuart Chambers,Richard H. Herbert,Sarah Christine Hobbs,Steven R. Thomas,Hugh M. Verrier,Alan P. Watt,Richard G. Ball +8 more
TL;DR: In this paper, the synthesis of (+)- and (-)-epibatidine (exo-2-(2-chloropyridin-5-yl)-7-azabicyclo[2.2.1]heptane) via reaction of 5-lithio-2-loropyridine with (+)-and (-)-N-BOC-7-AZA-1-one is described.
Journal ArticleDOI
Higher throughput bioanalysis by automation of a protein precipitation assay using a 96-well format with detection by LC-MS/MS.
TL;DR: Generic methodology for the automated preparation and analysis of drug levels in plasma samples within a drug discovery environment was achieved through the redesign of a protein precipitation assay to a microtiter plate format and the application of robotic liquid handling for performance of all transfer and pipetting steps.