Abstract
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.
MeSH terms
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Animals
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Female
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Humans
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Kinetics
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Oxytocin / antagonists & inhibitors*
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Oxytocin / metabolism
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Piperazines / chemistry*
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Piperazines / pharmacokinetics
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Piperazines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptors, Oxytocin / metabolism
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Structure-Activity Relationship
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Uterine Contraction / drug effects
Substances
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GSK221149A
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Piperazines
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Receptors, Oxytocin
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Oxytocin