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The discovery of GSK221149A: A potent and selective oxytocin antagonist

2007; Elsevier BV; Volume: 18; Issue: 1 Linguagem: Inglês

10.1016/j.bmcl.2007.11.008

1464-3405

John Liddle, Michael Allen, Alan D. Borthwick, David P. Brooks, David E. Davies, Richard M. Edwards, Anne M. Exall, C. Hamlett, Wendy R. Irving, Andrew M. Mason, Gerald P. McCafferty, Fabrizio Nerozzi, Simon Peace, Joanne Philp, Derek Pollard, Mark Pullen, Shaila Shabbir, Steve L. Sollis, Timothy D. Westfall, Pat M. Woollard, Charlene Wu, Deirdre M. B. Hickey,

Neuropeptides and Animal Physiology

Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat.