M
Michael Allen
Researcher at University of Exeter
Publications - 45
Citations - 862
Michael Allen is an academic researcher from University of Exeter. The author has contributed to research in topics: Oxytocin receptor & Oxytocin. The author has an hindex of 16, co-authored 42 publications receiving 774 citations. Previous affiliations of Michael Allen include GlaxoSmithKline & National Institute for Health Research.
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Journal ArticleDOI
The discovery of GSK221149A: A potent and selective oxytocin antagonist
John Liddle,Michael Allen,Alan D. Borthwick,David P. Brooks,David E. Davies,Richard M. Edwards,Anne M. Exall,Christopher Charles Frederick Hamlett,Wendy R. Irving,Andrew M. Mason,Gerald P. McCafferty,Fabrizio Nerozzi,Simon Peace,Joanne Philp,Derek Pollard,Mark Pullen,Shaila S. Shabbir,Steve L. Sollis,Timothy D. Westfall,Pat M. Woollard,Charlene Wu,Deirdre Mary Bernadette Hickey +21 more
TL;DR: Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A, which has been shown to inhibit oxytocarine contractions in the anaesthetised rat.
Journal ArticleDOI
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.
Alan D. Borthwick,John Liddle,Dave E. Davies,Anne M. Exall,Christopher Charles Frederick Hamlett,Deirdre Mary Bernadette Hickey,Andrew M. Mason,Ian Edward David Smith,Fabrizio Nerozzi,Simon Peace,Derek Pollard,Steve L. Sollis,Michael Allen,Patrick M. Woollard,Mark Pullen,Timothy D. Westfall,Dinesh Stanislaus +16 more
TL;DR: Epelsiban has low levels of intrinsic clearance against the microsomes of four species, good bioavailability and comparable potency to atosiban in the rat, but is 100-fold more potent than the latter in vitro and was negative in the genotoxicity screens with a satisfactory oral safety profile in female rats.
Journal ArticleDOI
2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: Identification, stereochemistry and initial SAR.
Paul G. Wyatt,Michael Allen,Alan D. Borthwick,Dave E. Davies,Anne M. Exall,Richard J. D. Hatley,Wendy R. Irving,Livermore David,Neil Derek Miller,Fabrizio Nerozzi,Steve L. Sollis,Anna Katrin Szardenings +11 more
TL;DR: The initial structure-activity relationship investigations and the determination of the stereochemistry of the most potent compounds are reported, covering efforts to discover orally active potent and selective oxytocin antagonists.
Journal ArticleDOI
Paracrine oxytocin and estradiol demonstrate a spatial increase in human intrauterine tissues with labor.
Andrew M. Blanks,Manu Vatish,Michael Allen,Graham Ladds,Norbert C. J. de Wit,Donna M. Slater,Steven Thornton +6 more
TL;DR: It is concluded that a significant increase in both OT and E2 occurs at the myometrial decidual interface with labor, and this increase is reflected in both the fundal and lower segments of the uterus.
Journal ArticleDOI
2,5-Diketopiperazines as Potent, Selective, and Orally Bioavailable Oxytocin Antagonists. 2. Synthesis, Chirality, and Pharmacokinetics
Alan D. Borthwick,Dave E. Davies,Anne M. Exall,Livermore David,Steve L. Sollis,Fabrizio Nerozzi,Michael Allen,Marion J. Perren,Shalia S Shabbir,Patrick M. Woollard,Paul G. Wyatt +10 more
TL;DR: The 2',4'-difluorophenyldiketopiperazine derivative 37 is a highly potent oxytocin antagonist against the human oxytocIn receptor that has >1000-fold selectivity over all three vasopressin receptors V1a, V2, and V1b.